Tag: 100-200

On January 20, 2017, Aruri, Hariprasad; Singh, Umed; Kumar, Mukesh; Sharma, Sumit; Aithagani, Sravan Kumar; Gupta, Vivek K.; Mignani, Serge; Vishwakarma, Ram A.; Singh, Parvinder Pal published an article.Recommanded Product: 685-91-6 The title of the article was Metal-free Cross-Dehydrogenative Coupling of HN-azoles with α-C(sp3)-H Amides via C-H Activation and Its Mechanistic and Application Studies. And the article contained the following:

A metal-free one step coupling reaction between various N-azole rings and diverse α-C(sp3)-H containing amides has been developed under oxidative reaction conditions. Com. available tetrabutylammonium iodide (TBAI) in the presence of tert-Bu hydroperoxide (TBHP), under neat reaction conditions, efficiently catalyzed the coupling. Various azole types, such as 1H-benzotriazoles, 1H-1,2,3-triazoles, 1H-1,2,4-triazoles, 1H-tetrazoles, 1H-pyrazoles, and 1H-benzimidazoles, and α-C(sp3)-H containing amides, such as N,N-dimethylacetamide, N,N-dimethylbenzamide, N-methylacetamide, N,N-diethylacetamide, N-methylpyrrolidine, and pyrrolidin-2-one, were successfully employed for the coupling. A series of designed and controlled experiments were also performed in order to study the involvement of the different intermediates. Based on the evidence, a plausible mechanism is also proposed. These novel, simple, rapid, attractive, and straightforward transformations open the way of the construction of novel highly functionalized N-azoles via direct covalent N-H bond transformations onto N-C bonds. This approach allows to the synthesis of complex mols. requiring number of steps using classical synthetic ways. In addition, the range of α-C(sp3)-H containing amide substrates is virtually unlimited highlighting the potential value of this simple system for the construction of complex heterocyclic mols., such as fused azole derivatives The experimental process involved the reaction of N,N-Diethylacetamide(cas: 685-91-6).Recommanded Product: 685-91-6

The Article related to dehydrogenative coupling azole amide, Heterocyclic Compounds (More Than One Hetero Atom): Other 5-Membered Rings, Two Or More Hetero Atoms and other aspects.Recommanded Product: 685-91-6

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On November 30, 2011, Suzdalev, K. F.; Den’kina, S. V. published an article.Recommanded Product: 2-(4-Methylbenzamido)acetic acid The title of the article was Synthesis of 1-(oxiran-2-ylmethyl)-1H-indole-3-carbaldehyde and its reaction with active methylene compounds. And the article contained the following:

Treatment of indole-3-carbaldehyde with epichlorohydrin gave 1-(oxiran-2-ylmethyl)-1H-indole-3-carbaldehyde, reaction of which with 1,3-dimethylbarbituric acid or malononitrile gave crotonic condensation products with retention of the oxirane ring. The structure of the reaction products with aroylglycines depends on the conditions. In acetic anhydride a simultaneous formation of an oxazolone ring and bisacylation of the oxirane fragment occurs; the use of Et chloroformate in the presence of triethylamine resulted in only the heterocyclization process. When treated with the cyclic amines (N-methylpiperazine or morpholine), opening of the oxazolone ring in the products occurs with formation of the corresponding amides. The experimental process involved the reaction of 2-(4-Methylbenzamido)acetic acid(cas: 27115-50-0).Recommanded Product: 2-(4-Methylbenzamido)acetic acid

The Article related to oxiranylmethylindolecarbaldehyde preparation reaction active methylene compound, indolecarbaldehyde oxiranylmethyl preparation reaction active methylene compound, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Recommanded Product: 2-(4-Methylbenzamido)acetic acid

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Shyamsundar, M.; Shamshuddin, S. Z. Mohamed published an article in 2019, the title of the article was Mo (VI)/ZrO2 coated on honeycomb monolith as solid acid green catalyst for the acetylation of substituted alcohols and amines under solvent free conditions.Synthetic Route of 685-91-6 And the article contains the following content:

Honeycomb (HC) monolith coated with solid acids such as Mo (VI)/ZrO2 (MZ) with different Mo loadings (2, 6 and 10%) have been prepared by wet impregnation method and characterized by NH3 -TPD, BET surface area, PXRD, ICPOES, SEM, TEM and EDAX techniques. These catalysts have been used as for the synthesis of O and N-acetylation reactions by the condensation of various alcs. with acetic anhydride under solvent free conditions in shorter times (20 min) at moderate temperature (70°C). Especially, 6% Mo (VI)/ZrO2 catalysts are found to be highly acidic and also resulted in high yields of O and N acetylated products up to ~99%. This methodol. offers several advantages such as excellent yields, easy procedure, mild and environmentally benign conditions. MZ catalysts are found to be economical, efficient and highly active, recyclable and reusable up to 6 reaction cycles without much loss of their activity. The experimental process involved the reaction of N,N-Diethylacetamide(cas: 685-91-6).Synthetic Route of 685-91-6

The Article related to molybdenum zirconia coated honeycomb monolith solid acid green catalyst, substituted alc acetylation, Industrial Organic Chemicals, Leather, Fats, and Waxes: Manufacture Of Industrial Organic Chemicals and other aspects.Synthetic Route of 685-91-6

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Zamani, Parisa; Khosropour, Ahmad R. published an article in 2016, the title of the article was A combination of natural deep eutectic solvents and microflow technology: a sustainable innovation for the tandem synthesis of 3-aminohexahydrocoumarins.Name: 2-(4-Methylbenzamido)acetic acid And the article contains the following content:

We describe herein the first, straightforward, green, and metal-free tandem continuous flow pseudo-four component reaction to form 3-aminohexahydrocoumarins using choline chloride-urea as a natural deep eutectic solvent. This technol. exhibited superior yields relative to the batch reactions. The experimental process involved the reaction of 2-(4-Methylbenzamido)acetic acid(cas: 27115-50-0).Name: 2-(4-Methylbenzamido)acetic acid

The Article related to eutectic microflow technol aminohexahydrocoumarin, Industrial Organic Chemicals, Leather, Fats, and Waxes: Manufacture Of Industrial Organic Chemicals and other aspects.Name: 2-(4-Methylbenzamido)acetic acid

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On March 30, 2017, Ma, Dawei; Yu, Qiang; Yuan, Junying; Xia, Hongguang; Cai, Dongpo; Wang, Kailiang; Zhang, Chen; Xia, Shanghua published a patent.Application of 16230-24-3 The title of the patent was 2,4-Diamino-5-(trifluoromethyl)pyridine-1,3-diaminobenzene-acrylamide derivatives as EGFR kinase inhibitors and their preparation, pharmaceutical compositions and use in the treatment of cancer. And the patent contained the following:

The invention provides 2,4-diamino-5-(trifluoromethyl)pyridine-1,3-diaminobenzene-acrylamide derivatives of formula I as EGFR kinase inhibitors and the preparation method and use thereof. Compounds of formula I wherein X and Y are independently N, CH; provided that X and Y are not CH at the same time; R is (un)substituted 5- to 7-membered heterocyclic ring, -NH-(un)substituted 5- to 7-membered heterocyclic ring, etc.; and their preparation method, as well as their use as EGFR kinase inhibitors in the treatment of cancer thereof, are claimed. Compounds of formula I were prepared by using condensation and deacylation as the key steps. All the invention compounds were evaluated for their EGFR inhibitory activity. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Application of 16230-24-3

The Article related to trifluoromethyl pyridine diaminobenzene acrylamide preparation egfr inhibitor treatment cancer, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Application of 16230-24-3

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On December 30, 2009, Aissaoui, Hamed; Boss, Christoph; Koberstein, Ralf; Siegrist, Romain; Sifferlen, Thierry published a patent.Name: (S)-2-Hydroxy-N-methyl-2-phenylacetamide The title of the patent was 5,6,7,8-Tetrahydroimidazo[1,5-a]pyrazine compounds as orexin receptor antagonists and their preparation, pharmaceutical compositions and use in the treatment of diseases. And the patent contained the following:

The invention relates to 5,6,7,8-tetrahydroimidazo[1,5-a]pyrazine derivatives of formula I and to the use of such compounds as medicaments, especially as orexin (OX) receptor antagonists. Compounds of formula I wherein R4 is C1-4 alkyl; when R3 is cyclopropyl, then R2 is halo, CF3, C1-4 alkyl and vinyl, R1 is substituted phenyl; when R3 is C3-6 cycloalkyl-C1-4 alkyl, then R2 is halo, R1 is substituted phenyl; when R3 is -SO2-C1-4 alkyl, then R2 is halo, R1 is substituted phenyl; when R3 is -S-C1-4 alkyl, then R2 is halo, CF3 and vinyl, R1 is substituted phenyl; when R3 is C1-4 alkyl, then R2 is -SO0-2-C1-4 alkyl, R1 is substituted phenyl; when R3 is C1-4 alkoxy, then R2 is CF3, R1 is substituted phenyl; when R3 is CF3, then R2 is C1-4 alkyl, R1 is substituted phenyl; when R3 is C1-4 alkyl, then R2 is halo, R1 is substituted phenyl; and their pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared via N-alkylation of 1-chloro-8-[2-(4-chloro-3-fluorophenyl)ethyl]-3-cyclopropyl-5,6,7,8-tetrahydroimidazo[1,5-a]pyrazine with toluene-4-sulfonic acid (S)-methylcarbamoylphenyl Me ester. All the invention compounds were evaluated for their OX receptor antagonistic activity. From the assay, it was determined that II exhibited the IC50 values of 43 nM and 11 nM against OX1 and OX2, resp. The experimental process involved the reaction of (S)-2-Hydroxy-N-methyl-2-phenylacetamide(cas: 65645-88-7).Name: (S)-2-Hydroxy-N-methyl-2-phenylacetamide

The Article related to tetrahydro imidazopyrazine compound preparation orexin receptor antagonist treatment disease, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Name: (S)-2-Hydroxy-N-methyl-2-phenylacetamide

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On January 27, 2022, Wu, Hao; Wu, Wenmao; Li, Ling; Zhang, Zhan; Wang, Feng; Yuan, Ding; Wu, Yunfei; Chen, Qiang; Han, Han; Guo, Jing; Lan, Hong; Ding, Lieming; Wang, Jiabing published a patent.Category: amides-buliding-blocks The title of the patent was Piperidine-spiro-fused heterocyclic compounds as SHP2 inhibitors and their preparation, pharmaceutical compositions and use in the treatment of diseases. And the patent contained the following:

The invention relates to piperidine-spiro-fused heterocyclic compounds of formula I, which are serving as an Src homol. region 2-containing protein tyrosine phosphatase 2 (SHP2) inhibitors, as well as to their pharmaceutical compositions thereof, the preparation method therefor, and the use in treating an SHP2 mediation disease. The compounds of formula I exert effects by means of participating in the regulation of multiple processes such as cell proliferation, apoptosis, migration, and angiogenesis. Compounds of formula I wherein the dotted double bond is either a single bond, or a double bond; ring A is (un)saturated 5- to 10-membered (hetero)cyclic ring; ring C is (un)saturated 5- to 10-membered heterocyclic ring, C6-10 aryl, 5- to 10-membered heteroaryl; each Rc is independently H, halo, CN, NO2, SF5, C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, etc.; two of the Rc may be taken together with the atom attached to form C3-8 cycloalkyl, 3- to 10-membered heterocyclic ring, C6-10 aryl, 5- to 10-membered heteroaryl, etc.; T is (CRc1Rc2)0-3; Rc1 and Rc2 are independently H, halo, C1-4 alkly, -OR5; Rc1Rc2 may be taken together with the atom attached to form C3-6 cycloalkyl, 3- to 6-membered heterocyclic ring; each R1 is independently H, halo, CN, NO2, C1-6 alkyl, C2-4 alkenyl, C2-4 alkynyl, C3-6 cycloalkyl, etc.; X is O, NH and derivatives, SO0-2, CO, -CO-O-, -CO-NH- and derivatives, etc.; M is O, NH and derivatives, (un)substituted CH; Y1 and Y2 are independently NH and derivatives, (un)substituted CH; each R4 is independently H, halo, CN, NO2, C1-8 alkyl, C2-8 alkenyl, etc.; R5 is H, C1-8 alkyl, C2-8 alkenyl, C2-8 alkenyl, etc.; and their pharmaceutically acceptable salts, deuterium,stereoisomers, chelates, prodrugs as SHP2 inhibitors in the treatment of diseases thereof, are claimed. Example compound II was prepared by using spirocyclization, imination, reduction, cross-coupling as the key steps. All the invention compounds were evaluated for their SHP2 inhibitory activity. The experimental process involved the reaction of 2-Fluoro-4-hydroxybenzamide(cas: 1133122-96-9).Category: amides-buliding-blocks

The Article related to piperidine spiro fused heterocyclic preparation shp2 inhibitor treatment disease, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Category: amides-buliding-blocks

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On March 22, 2022, Chen, Yong; Zhuang, Xiaoxiao published a patent.Related Products of 16230-24-3 The title of the patent was Preparation of rociletinib as epidermal cell growth factor receptor mutation inhibitor. And the patent contained the following:

The present invention relates to preparation of rociletinib as epidermal cell growth factor receptor mutation inhibitor. In particular, the preparation method comprises of following steps; (a) substitution reaction between 1-[4-(4-amino-3-methoxyphenyl)piperazin-1-yl]ethan-1-one and di-tert-Bu dicarbonate under the action of a base and an organic solvent to obtain tert-Bu (4-(4-acetylpiperazin-1-yl)-2-methoxyphenyl)carbamate; (b) substitution reaction of step (a) product and 2,4-dichloro-5-(trifluoromethyl)pyrimidine under the action of a base and an organic solvent to obtain tert-Bu (4-(4-acetylpiperazin-1-yl)-2-methoxyphenyl)(4-chloro-5-(trifluoromethyl)pyrimidin-2-yl)carbamate; (c) substitution reaction of step (b) product and N-(3-aminophenyl)prop-2-enamide under the action of base and an organic solvent to obtain tert-Bu (4-(4-acetylpiperazin-1-yl)-2-methoxyphenyl)(4-((3-acrylamidophenyl)amino)-5-(trifluoromethyl)pyrimidin-2-yl)carbamate, and (d) hydrolysis reaction reaction of step (c) product under the action of an acid and an organic solvent to obtain the compound rociletinib. The preparation method of the epidermal cell growth factor receptor mutation inhibitor of the present invention has the advantages that the raw materials required for each step are cheap, easy to purchase, and the synthesis route is short, no isomers are produced, the intermediates are easy to sep. and purify, no column chromatog. is required, and the obtained product has high purity, high atom utilization, high yield, convenient purification, safe and simple reaction, and can be industrially produced. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Related Products of 16230-24-3

The Article related to rociletinib preparation epidermal cell growth factor receptor mutation inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Related Products of 16230-24-3

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On January 13, 2022, Steadman, David; Atkinson, Benjamin N.; Zhao, Yuguang; Willis, Nicky J.; Frew, Sarah; Monaghan, Amy; Patel, Chandni; Armstrong, Emma; Costelloe, Kathryn; Magno, Lorenza; Bictash, Magda; Jones, E. Yvonne; Fish, Paul V.; Svensson, Fredrik published an article.Reference of 2-(4-Methylbenzamido)acetic acid The title of the article was Virtual Screening Directly Identifies New Fragment-Sized Inhibitors of Carboxylesterase Notum with Nanomolar Activity. And the article contained the following:

Notum is a neg. regulator of Wnt signaling acting through the hydrolysis of a palmitoleoylate ester, which is required for Wnt activity. Inhibitors of Notum could be of use in diseases where dysfunctional Notum activity is an underlying cause. A docking-based virtual screen (VS) of a large com. library was used to short-list 952 compounds for exptl. validation as inhibitors of Notum. The VS was successful with 31 compounds having an IC50 < 500 nM. A critical selection process was then applied with two clusters and two singletons selected for hit validation. Optimization of I guided by structural biol. identified potent inhibitors of Notum activity that restored Wnt/β-catenin signaling in cell-based models. The [1,2,4]triazolo[4,3-b]pyridazin-3(2H)-one series represent a new chem. class of Notum inhibitors and the first to be discovered by a VS campaign. These results demonstrate the value of VS with well-designed docking models based on X-ray structures. The experimental process involved the reaction of 2-(4-Methylbenzamido)acetic acid(cas: 27115-50-0).Reference of 2-(4-Methylbenzamido)acetic acid

The Article related to triazolopyridazinone preparation carboxylesterase notum inhibitor screening, Heterocyclic Compounds (More Than One Hetero Atom): Other 6-Membered Rings, Three Or More Hetero Atoms and other aspects.Reference of 2-(4-Methylbenzamido)acetic acid

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On July 3, 2008, Aissaoui, Hamed; Boss, Christoph; Gude, Markus; Koberstein, Ralf; Sifferlen, Thierry published a patent.HPLC of Formula: 65645-88-7 The title of the patent was Preparation of 5,6,7,8-tetrahydro-imidazo[1,5-a]pyrazine derivatives as orexin receptor antagonists. And the patent contained the following:

Title compounds represented by the formula I [wherein X = CH2 or O; R1 = independently phenyl; R2 = alkyl, alkenyl, halo, etc.; R3 = alkyl, alkoxymethyl or halo; R4 = alkyl; and pharmaceutically acceptable salts thereof] were prepared as orexin (OX) receptor antagonists. For example, II was provided in a multi-step synthesis starting from Knoevenagel condensation of 3,4-dimethylbenzaldehyde with malonic acid. I showed antagonistic activity on OX1 and OX2 receptors in intracellular calcium measurements. The experimental process involved the reaction of (S)-2-Hydroxy-N-methyl-2-phenylacetamide(cas: 65645-88-7).HPLC of Formula: 65645-88-7

The Article related to tetrahydroimidazopyrazine preparation orexin receptor antagonists, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.HPLC of Formula: 65645-88-7

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics