Category: amides-buliding-blocks

On April 6, 2016, Fu, Kaiyong; Li, Hua; Zhang, Changjiang published a patent.Category: amides-buliding-blocks The title of the patent was Process for preparation of tyrosine kinase inhibitor Rociletinib. And the patent contained the following:

The invention relates to a method for preparing tyrosine kinase inhibitor Rociletinib, namely N-[3-[[2-[[4-(4-acetyl-1-piperazinyl)-2-p-methoxyphenyl]amino]-5-(trifluoromethyl)-4-pyrimidinyl]amino]phenyl]-2-acrylamide, with a total yield of 60-65%. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Category: amides-buliding-blocks

The Article related to preparation tyrosine kinase inhibitor rociletinib, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Category: amides-buliding-blocks

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

On March 9, 2016, Li, Yao; Wei, Yonggang; Zhang, Guobiao; Chen, Lei; Zhang, Xiaobo; Qiu, Guanpeng; Xu, Bo published a patent.HPLC of Formula: 16230-24-3 The title of the patent was Pyrimidine derivative, its preparation method and pharmaceutical application. And the patent contained the following:

The invention disclosed a kind of pyrimidine derivative, its preparation method and pharmaceutical application. The claimed pyrimidine derivative i shown in structure I (M1,M2 = (un)substituted Michael receptor groups; ring D = 6-10 member heterocycle, ring E,A = C6-10 ring, or 4-10 member heterocycle, etc.; ring B,C = (un)substituted 4-7 heterocycle, or not exist; W1,W2 = Nh, O or S; W3,W4 = NH, O, S or not exist). The claimed compound is prepared via multiple steps (procedure given). The obtained compound, its stereoisomer, hydrate, metabolite, solvate, pharmaceutically acceptable salt, eutectic, or prodrug, can be used as EGFR inhibitor for treating or prevention hyperproliferative diseases such as brain tumors, non-small cell lung cancer, squamous cell cancer, bladder cancer, pancreatic cancer, colon cancer, breast cancer, ovarian cancer, cervical cancer, endometrial cancer, colorectal cancer, renal cancer, esophageal adenocarcinoma, esophageal squamous cell carcinoma, solid tumors, Non-Hodgkin’s lymphoma, liver cancer, lung cancer, skin cancer, thyroid cancer, head and neck cancer, prostate cancer, glioma and nasopharyngeal carcinoma. 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 pyrimidine derivative preparation egfr inhibitor, 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

On January 4, 2018, Kim, In Woo; Han, Mi Ryeong; Yoo, Jakyung; Oh, Yun Ju; Kim, Ji Duck; Kim, Nam Youn; Jun, Sun Ah; Lee, Jun Hee; Park, Joon Seok published a patent.Electric Literature of 16230-24-3 The title of the patent was Pyrazolopyrimidine derivatives as kinase inhibitor and their preparation. And the patent contained the following:

The invention relates to a pyrazolopyrimidine derivative of formula I, or a pharmaceutically acceptable salt thereof. The compound according to the invention can be usefully used for the prevention or treatment of diseases which are associated with kinase inhibitory actions. Compounds of formula I wherein R1 is (un)substituted C6-10 aryl and (un)substituted C2-10 heteroaryl; R2 is H, C1-4 alkyl and halo; R3 is (un)substituted C1-4 alkyl, (un)substituted C2-6 alkenyl and (un)substituted C2-6 alkynyl; X1 is CR4 and N; R4 is H, C1-4 alkyl and halo; X2 is CR5 and N; R5 is H, C1-4 alkyl, C1-4 alkoxy, halo, etc.; X3 is NH and derivatives, O and S; X4 is CH and N; X5 is a bond and NH; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by amination of 2,4-dichloro-7H-pyrrolo[2,3-d]pyrimidine with tert-Bu (R)-3-aminopiperidin-1-carboxylate followed by Boc-deprotection; the resulting (R)-2-chloro-N-(piperidin-3-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine hydrochloride underwent N-acylation with acryloyl chloride followed by amination with 4-(4-methylpiperazin-1-yl)aniline to give compound II. The invention compounds were evaluated for their kinase inhibitory activity. From the assay, it was determined that compound II exhibited IC50 values of 3.73 nM and 10.7 nM towards JAK3 and BTK, resp. 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 pyrazolopyrimidine preparation kinase inhibitor, 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 11, 2018, Zhang, Xiaoqing; Song, Zhichun; Bao, Jinyuan published a patent.Application of 16230-24-3 The title of the patent was Preparation of pyrimidine derivatives useful as IDO inhibitors. And the patent contained the following:

The invention relates to pyrimidine derivatives of formula I, and their pharmaceutically acceptable salts, isomers, racemates, diastereoisomers and pharmaceutical composition thereof, method for their preparation and their use for the treatment of diseases related to indoleamine 2,3-dioxygenase (IDO), specifically in the treatment of tumors, Alzheimer’s disease, depression, cataract, etc. Compounds of formula I, wherein R2 is halo, H, (un)substituted Ph, 4-pyrazolyl, etc.; R is (un)substituted C5-12aryl, C1-6alkyl, NH2, 1-substituted-4-pyrazolyl, etc.; W is 4-fluoroanilino, C1-6alkoxy, cyclopentylamino, 4- to 8-membered heterocycle containing at least one N, and their pharmaceutically acceptable salts, are claimed. Example compound II was prepared via a multistep procedure (procedure given). All the invention compounds were evaluated for their IDO inhibitory activity. From the assay, it was determined that example compound II exhibited 46 % and 26 % inhibition towards IDO1 at 10 μM and 1 μM resp. Pharmacokinetic behaviors of the invented compounds in rats are studied, and the results show that the compound of the present invention has a significant pharmacokinetic absorption effect and a good clin. application prospect. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Application of 16230-24-3

The Article related to pyrimidine derivative preparation ido inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Application of 16230-24-3

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

On January 15, 2015, Hu, Shaojing; Liu, Xiangyong; Bai, Jinlong; Long, Wei published a patent.COA of Formula: C9H10N2O The title of the patent was Preparation of pyrimidines as protein tyrosine kinase modulators. And the patent contained the following:

Heterocyclic pyrimidine compounds that modulate mutant-selective epidermal growth factor receptor (EGFR) and ALK kinase activity are disclosed. More specifically, the invention provides pyrimidines which inhibit, regulate and/or modulate kinase receptor, particularly in selectively modulation of various EGFR mutant activity and ALK kinase activity have been disclosed. Pharmaceutical compositions comprising the pyrimidine derivative,and methods of treatment for diseases associated with protein kinase enzymic activity, particularly EGFR or ALK kinase activity including non-small cell lung cancer comprising administration of the pyrimidine derivative are disclosed. Compounds I [X = absent, O, S, or NR16; R16 = H or alkyl; Y = halogen, OH, NH2, CN, N3, NO2, or (un)substituted alkyl; Z = O, S, NR20, or CR20R21; and each R20 or R21 independently = H, halogen, (un)substituted alkyl, or alkoxy; R1 = hydroxy, alkyl, haloalkyl, aryl, arylalkyl, etc.; R2 = H, F, or alkyl; or R3 = H, halogen, or a 5 or 6 member heterocyclic ring; R4 = H, alkoxy, alkenyloxy, cycloalkyloxy, halogen, etc.; R5 = H, F, alkyl, haloalkyl, alkoxy, etc.; R6 = H, halo, CN, NO2, cycloalkyl, etc.; R7 = H, halo, alkyl, alkoxy, alkenyloxy, etc.], and their pharmaceutically acceptable salts, are prepared and disclosed. Thus, e.g., II was prepared by. Compound II showed IC50 value of 27.9 nM in ALK assay, 44.3 nM in EGFR (ErB1) L858R assay and 4.08 nM in EGFR (ErbB1) T790M L858R assay. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).COA of Formula: C9H10N2O

The Article related to pyrimidine preparation protein tyrosine kinase, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.COA of Formula: C9H10N2O

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

On April 19, 2017, Ma, Xiaodong; Song, Anran; Wang, Luhong; Liu, He; Zhang, Baojing; Wang, Changyuan; Meng, Qiang; Shu, Xiaohong; Zhen, Yuhong; Liu, Kexin published a patent.Category: amides-buliding-blocks The title of the patent was Preparation of distyryl pyrimidine derivatives as antitumor agents. And the patent contained the following:

Title compounds I [wherein X = NH or O; R1 = Cl, F, CF3, or NO2; R2 = H, Me, OMe, or CN; R3 = (R4)n, n is 1 to 4, R4 is H, Me, OMe, OH, F, Cl, or Br], and their pharmaceutically acceptable salts thereof, were prepared as EGFR inhibitors useful as antitumor agents. Thus, the invention compound II was prepared and gave an EGFR inhibition IC50 value of 51.34nmmol. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Category: amides-buliding-blocks

The Article related to distyryl pyrimidine antitumor egfr preparation, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Category: amides-buliding-blocks

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

On May 16, 2018, Na, Yun Su; Bang, Geuk Chan; Park, Jun Seok published a patent.Related Products of 16230-24-3 The title of the patent was Preparation of novel pyrrolopyrimidine derivatives as BTK inhibitors and pharmaceutical composition comprising the same. And the patent contained the following:

The invention relates to a compound of formula I or a pharmaceutically acceptable salt thereof, and the compound according to the invention can be usefully used for the prevention or treatment of diseases in which the BTK inhibitory action is beneficial. Compounds of formula I wherein X is NH and O; L is a bod and CO; R is H, (un)substituted C6-10 aryl and (un)substituted C3-10 heteroaryl; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for their BTK inhibitory activity. From the assay, it was determined that compound II exhibited IC50 value of 20.9 n< and 100 % inhibition at 1 μM. 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 pyrrolopyrimidine preparation btk inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Related Products of 16230-24-3

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

A. K., Ajeesh Kumar; Bodke, Yadav D.; Gowda, Ashwath N.; Sambasivam, Ganesh; Bhat, Kishore G. published an article in 2017, the title of the article was Design, Synthesis, and Evaluation of the Anticancer Properties of a Novel Series of Imidazolone Fused Pyrazolo[1,5-a]pyrimidine Derivatives.Name: 2-(4-Methylbenzamido)acetic acid And the article contains the following content:

A novel series of imidazolone fused pyrazolo[1,5-a]pyrimidine derivatives has been designed and synthesized using a convergent approach, and the structures of these compounds were confirmed by 1H NMR, 13C NMR, ESI-MS, and IR analyses. These new compounds were tested for their in vitro antiproliferative activity using an 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay. Out of the 20 derivatives prepared in the current study, some compounds exhibited good anticancer activities tested against HeLa cells and HepG2 cells. However, the in vitro anticancer activity of compound I against HeLa, HepG2, and MCF-7 cell lines is superior to the marketed drugs Paclitaxel and SAHA. 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 imidazolone fused pyrazolopyrimidine preparation anticancer activity, 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

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

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