Month: November 2022

On May 31, 2017, Ma, Xiaodong; Zhao, Dan; Wang, Luhong; Qu, Menghua; Huang, Shanshan; Wang, Changyuan; Shu, Xiaohong; Liu, Kexin published a patent.Computed Properties of 16230-24-3 The title of the patent was Sulfoamido pyrimidine compound as Bruton tyrosine kinase inhibitor and its preparation. And the patent contained the following:

The invention relates to sulfoamido pyrimidine compound of formula I as Bruton tyrosine kinase inhibitor and its preparation Compounds I, wherein R1 is Cl, F, nitro or trifluoromethyl; R2 is H, Me, methoxy or Cl; X is NH or O; R3 is Me, methoxy, or F; their pharmaceutically acceptable salts, are claimed. The inventive compound can inhibit Bruton tyrosine kinase, so as to treat tumors, especially Burkitts lymphoma, disseminated large B cell lymphoma, follicular lymphoma or chronic lymphocytic leukemia. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Computed Properties of 16230-24-3

The Article related to sulfoamido pyrimidine preparation bruton tyrosine kinase inhibitor treatment cancer, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Computed Properties of 16230-24-3

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

On January 25, 2019, Sun, Xiuli; Chi, Fuyun; Shu, Xiaohong; Ma, Xiaodong; Sun, Fangfang; Mo, Guangquan; Shangguan, Xinghe; Cai, Wei; Wang, Yao; Jiang, Feng; Wang, Yi; Sun, Guozhen published a patent.Electric Literature of 16230-24-3 The title of the patent was Pyrimidothiazole heterocyclic compound, composition, and used for treating lymphocytic leukemia. And the patent contained the following:

A pyrimidothiazole heterocyclic compound I and II having capability of treating tumor diseases by inhibiting JAK3 tyrosine kinase, Burkitt’s lymphoma, follicular lymphoma or chronic lymphocytic leukemia, and diffusing large B-cell lymphoma is provided. In compounds I and II, X is selected from the group consisting of NH or oxygen, and R1 is hydrogen, chlorine, Me, and fluorine or methoxy group;. For instance, the invention compound I (X = O; R1 = H) was prepared via substitution of 2,4-dichloro-thieno[3,2-d]pyrimidine with N-(3-hydroxyphenyl)-2-propenamide followed by substitution with 4-[3-(4-morpholinyl)propoxy]-benzenamine. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Electric Literature of 16230-24-3

The Article related to pyrimidothiazole heterocyclic antitumor leukemia lymphoma jak inhibitor preparation, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Electric Literature of 16230-24-3

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

On May 21, 2019, Li, Jiarui; Xu, Ruyi; Cao, Qinyuan published a patent.HPLC of Formula: 16230-24-3 The title of the patent was Anti-tumor compound, and its preparation method and application in preparing drug for treating myelocytic leukemia. And the patent contained the following:

The invention relates to N-(3-((5-chloro-2-((4-((4-hydroxypiperidin-1-yl)methyl)phenyl)amino)pyrimidin-4-yl)amino)phenyl)acrylamide I (named as BY4009) and its pharmaceutically acceptable salts (sulfate, pyrosulfate, etc.). Compound I was prepared starting from 1-(bromomethyl)-4-nitrobenzene, 4-hydroxypiperidine, and 3-nitroaniline by using benzylation, reduction, amidation and amination as the key steps. A pharmaceutical composition comprises the anti-tumor compound or its pharmaceutically acceptable salt, and pharmaceutically acceptable carrier. The pharmaceutical composition has application in preparing drug for treating tumor (myelocytic leukemia) by inhibiting BTK Tyrosine kinase phosphorylation. The anti-tumor compound has new mechanism of action, and is more effective. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).HPLC of Formula: 16230-24-3

The Article related to piperidinyl pyrimidinyl phenyl acrylamide preparation btk treatment myelocytic leukemia, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.HPLC of Formula: 16230-24-3

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

Chandraprakash, B.; Sarangapani, M. published an article in 2021, the title of the article was Synthesis, characterization, anticancer and antibacterial activity of 4-(benzylidene)-1-(pyrimidin-2-amino)-2-(p-tolyl)-1, 4-dihydro-4H-imidazol-5-one.Name: 2-(4-Methylbenzamido)acetic acid And the article contains the following content:

In present study, conventional synthesis of 4-(benzylidene)-1-(pyrimidin-2-amino)-2-(p-tolyl)-1, 4-dihydro-4H-imidazol-5-ones I [R = H, Me, Cl, etc.; R1 = H, MeO, NO2] was performed. All the synthesized products I were purified through column chromatog. and structures of these compounds were characterized by IR, 1H NMR and mass spectral data. All the final compounds I were screened for their anticancer and antibacterial activity and their efficacy were matched with standard drugs. The synthesized compounds I [R = Me, NO2, MeO, Br; R1 = H, MeO] showed good anticancer activities whereas others exhibited significant activities. The compounds I [R = Cl, MeO, NO2; R1 = H, MeO] has showed maximum antibacterial activity compare with streptomycin as a standard drug. 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 benzylidene pyrimidinyl amino tolyl dihydroimidazolone preparation antibacterial antitumor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Name: 2-(4-Methylbenzamido)acetic acid

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

Sanad, Sherif M. H.; Ahmed, Ahmed A. M.; Mekky, Ahmed E. M. published an article in 2020, the title of the article was Efficient synthesis and molecular docking of novel antibacterial pyrimidines and their related fused heterocyclic derivatives.Product Details of 79-07-2 And the article contains the following content:

3-(Benzo[d][1,3]dioxol-5-yl)-1-(thiophen-2-yl)prop-2-en-1-one (chalcone) reacted with thiourea and 6-amino-2-thioxo-2,3-dihydropyrimidin-4(1H)-one to give the corresponding 3,4-dihydro-1H-pyrimidine-2-thione and 2-thioxo-1H-pyrido[2,3-d]pyrimidin-4-one. Then, these compounds reacted with the appropriate hydrazonyl chlorides 4-R1C6H4NHN=C(Cl)R [R = C(O)Me, CO2Et; R1 = H, Me] in dioxane in presence of triethylamine to afford corresponding 1,5-dihydro-[1,2,4]triazolo[4,3-a]pyrimidines I [R = C(O)Me, CO2Et; R1 = H, Me] and their related fused pyridines II. Moreover, chalcone was cyclocondensed with 2-cyanothioacetamide to give corresponding 2-thioxo-1H-pyridine-3-carbonitrile, which was used as key synthon to synthesize fused heterocyclic compounds III [R2 = C(O)NH2, R3 = NH2; R2R3 = C(O)NHC(S)NH, C(O)NHC(O)NH, C(O)NHCH=N, C(O)NHC(Me)=N, C(O)NHC(SMe)=N]. The compound III [R2R3 = C(O)NHC(SMe)=N] reacted with appropriate hydrazonyl chlorides in dioxane in presence of triethylamine to yield corresponding pyrido[3′,2′:4,5]thieno[3,2-d][1,2,4]triazolo[4,3-a]pyrimidines IV [R = C(O)Me, CO2Et; R1 = H, Me]. Study of the in vitro antimicrobial activities of newly synthesized pyrimidines against different pathogenic bacterial and fungal strains were performed. The compound III [R2R3 = C(O)NHCH=N] showed the highest inhibitory activity against all bacteria with MIC values of 3.9, 7.81, 7.81, and 15.62μg/mL, resp., against Escherichia coli, Klebsiella pneumonia, Staphylococcus aureus and Streptococcus mutans, resp., as compared to reference drugs. Mol. docking was studied to predict the optimized conformation of pyrimidines as active ligands against Escherichia coli alk. phosphatase. The experimental process involved the reaction of 2-Chloroacetamide(cas: 79-07-2).Product Details of 79-07-2

The Article related to pyrimidine preparation antibacterial antifungal docking pharmacokinetic cytotoxicity human, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Product Details of 79-07-2

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

On April 13, 2016, Yao, Li published a patent.Quality Control of N-(3-Aminophenyl)acrylamide The title of the patent was Preparation of pyrimidine derivatives as EGFR and ALK kinase inhibitors for treatment of cancer. And the patent contained the following:

The present invention discloses compounds represented by formula I [wherein R1 and R2 are selected from H, halogen, cyano, etc.; R3 is selected from H, halogen, substituted or unsubstituted C1-C6 alkyl and C3-C8 cycloalkyl; R are independently selected from H, halo, CN, OH, NH2, etc.; X and Y are independently selected from CH, C-halo, C-CN, N, etc. with the proviso that at least one of X and Y is N; and so on] or their pharmaceutically acceptable salts, enantiomers, diastereomers, tautomers, solvates, polymorphs or prodrugs, and preparation method and pharmaceutical application thereof. For example, compound II was prepared in a multi-step synthesis. The compounds of the present invention have good kinase inhibitory activity, particularly on EGFR and ALK kinases and mutants thereof, and have good prospect in medicine for the treatment of cancer. (assay data given). The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Quality Control of N-(3-Aminophenyl)acrylamide

The Article related to preparation pyrimidine derivative human egfr alk kinase inhibitors, treatment cancer antitumor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Quality Control of N-(3-Aminophenyl)acrylamide

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

Gobouri, Adil A. H. published an article in 2020, the title of the article was Synthetic access of new 6-purineselenyl and 8-(1,3,4-thiadiazolyl)-7-benzyl-1, 3-dimethyl-1H-purine-2,6-(3H,7H)-dione derivatives.Name: 2-Chloroacetamide And the article contains the following content:

New 6-purineselenyl I (X = CN, C(O)2Et, CONH2), 1,3,4-thiadiazols bearing 7-benzyl-1,3-dimethyl-1H-purine-2,6-(3H,7H)-diones and (8-[2-(3-phenyl-5-substituted-1,3,4-thiadiazol-2(3H)-ylidene)hydrazinyl)-7-benzyl-1,3-dimethyl]-1H-purine-2,6-(3H,7H)-diones derivatives II [R = Ph, C(O)Me, OC(O)Et, C(O)NHC6H5] were synthesized. The structures of the newly synthesized compounds were elucidated by spectroscopic methods (1H-NMR, 13C-NMR, and MS spectrometry) and elemental anal. The experimental process involved the reaction of 2-Chloroacetamide(cas: 79-07-2).Name: 2-Chloroacetamide

The Article related to selenylpurine thiadiazole preparation, purinedione dimethyl hydrazinyl thiadiazolylidene preparation, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Name: 2-Chloroacetamide

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

On March 5, 2020, Krainc, Dimitri; Silverman, Richard B.; Zheng, Jianbin published a patent.SDS of cas: 16230-24-3 The title of the patent was Preparation of pyrrolopyrimidine compounds and uses thereof for modulating glucocerebrosidase activity. And the patent contained the following:

The invention relates to preparation of new small mols. having a pyrrolopyrimidine (I) core structure and the uses thereof for modulating glucocerebrosidase activity. Compounds I wherein m is o-6; R1 is aryl, heteroaryl, etc.; R2 is C1-6 alkyl or pyridinyl, are claimed. The example compound II was prepared via 3-step synthesis (procedure given). Also disclosed are pharmaceutical compositions comprising the small mols. which may be administered in methods of treating diseases or disorders associated with glucocerebrosidase activity, including neurol. diseases and disorders such as Gaucher’s disease and Parkinson’s disease. Compounds I may be utilized to generate activated glucocerebrosidase. The activated glucocerebrosidase can be administered in enzyme replacement therapy and/or utilized in screening assays for new small mols. that bind to the activated glucocerebrosidase and/or modulate the activity of the activated glucocerebrosidase. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).SDS of cas: 16230-24-3

The Article related to pyrrolopyrimidine preparation glucocerebrosidase modulator neurodegenerative metabolic disease treatment, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.SDS of cas: 16230-24-3

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

On December 3, 2021, Wu, Xiaoyun; Li, Qinlan; Guo, Qian; Wan, Shanhe; Li, Zhonghuang; Zhang, Jiajie published a patent.Formula: C9H10N2O The title of the patent was Preparation of dioxopiperidinyl-isoindolyl-alkylamidophenylamino-pyrimidinylaminophenyl piperazinyl-oxopentanamide derivative and application thereof. And the patent contained the following:

The present invention relates to the preparation of dioxopiperidinyl-isoindolyl-alkylamidophenylamino-pyrimidinylaminophenyl piperazinyl-oxopentanamide derivative and application thereof. In particular, the dioxopiperidinyl-isoindolyl-alkylamidophenylamino-pyrimidinylaminophenyl piperazinyl-oxopentanamide derivative I (wherein, L contains at least one of an alkyl group, a carbonyl group, an ether bond or an amine group) were prepared The inventive compound can be used as an EFGR inhibitor, has strong inhibitory activity against the cell line H1975 with high expression of EGFRL858R/T790M, and can effectively inhibit the growth of lung cancer cells, which can be used for preparing drugs for treating, preventing, delaying, assisting in treating or treating diseases related to EGFR activity and drugs for treating tumor diseases. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Formula: C9H10N2O

The Article related to dioxopiperidinyl isoindolyl alkylamidophenylamino piperazinyl oxopentaneamide preparation efgr inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Formula: C9H10N2O

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

On March 31, 2019, Spranitz, Peter; Soregi, Petra; Botlik, Bence Bela; Berta, Mate; Soos, Tibor published an article.Name: N,N-Diethylacetamide The title of the article was Organocatalytic Desymmetrisation of Fittig’s Lactones: Deuterium as a Reporter Tag for Hidden Racemisation. And the article contained the following:

Highly enantioselective desymmetrisation of Fittig’s lactones with alcs. was promoted by bifunctional cinchona squaramides to yield corresponding glutaric acid derivatives I [R = Me, cyclohexyl, Ph, etc.]. The reactions were carried out with monodeuterated methanol to detect possible hidden racemization of the stereogenic center. Current evidence suggested that racemization was not a relevant process for most substrates, partial erosion of enantioselectivity was only detected with ortho-substituted aryl derivates. The resultant glutaric acid derivatives possess a scaffold that was common in natural products and the compounds were also useful chiral building blocks for further synthetic endeavours. The experimental process involved the reaction of N,N-Diethylacetamide(cas: 685-91-6).Name: N,N-Diethylacetamide

The Article related to glutaric acid derivative enantioselective preparation, bicyclic fittig lactone organocatalytic desymmetrisation, Aliphatic Compounds: Esters, Linear Anhydrides, Acyl Peroxides, and Acyl Halides and other aspects.Name: N,N-Diethylacetamide

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