Category: 16230-24-3

On May 4, 2017, Xu, Xuenong published a patent.Related Products of 16230-24-3 The title of the patent was Process for preparation of Rociletinib. And the patent contained the following:

This invention discloses a process for the preparation of Rociletinib, which comprises condensation reaction of 5-trifluoromethyluracil with 4-(4-acetyl-piperazin-1-yl)-2-methoxyaniline to obtain 2-[[4-(4-acetyl-piperazin-1-yl)-2-methoxyphenyl]amino]-5-(trifluoromethyl)-pyrimidin-4-one, followed by halogenation to obtain 2-[[4-(4-acetyl-piperazin-1-yl)-2-methoxy phenyl]amino]-5-(trifluoromethyl)-4-halo-pyrimidine, and amination with N-(3-aminophenyl)-2-acrylamide to obtain title product. The process has the advantages of easily available raw materials, simple procedures, low cost, etc. 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 preparation rociletinib condensation reaction halogenation amination, 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

On December 30, 2015, Xu, Xuenong published a patent.COA of Formula: C9H10N2O The title of the patent was Process for preparation of Rociletinib. And the patent contained the following:

This invention discloses a process for the preparation of Rociletinib, which comprises condensation reaction of 5-trifluoromethyluracil with 4-(4-acetyl-piperazin-1-yl)-2-methoxyaniline to obtain 2-[[4-(4-acetyl-piperazin-1-yl)-2-methoxyphenyl]amino]-5-(trifluoromethyl)-pyrimidin-4-one, followed by halogenation to obtain 2-[[4-(4-acetyl-piperazin-1-yl)-2-methoxy phenyl]amino]-5-(trifluoromethyl)-4-halo-pyrimidine, and amination with N-(3-aminophenyl)-2-acrylamide to obtain title product. The process has the advantages of easily available raw materials, simple procedures, low cost, etc. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).COA of Formula: C9H10N2O

The Article related to preparation rociletinib condensation reaction halogenation amination, 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 October 2, 2018, Yuan, Hong; Li, Si; Zhao, Jingyuan; Wu, Xiangdong; Wang, Xiaoxi; Wang, Nan; Yao, Bingjie; Zhao, Dan; Yao, Yao; Sun, Xiuli; Ma, Xiaodong published a patent.Safety of N-(3-Aminophenyl)acrylamide The title of the patent was Pyrimidine compound, composition and its application in treatment of lymphoma leukemia. And the patent contained the following:

The invention disclosed a kind of pyrimidine derivative, its preparation method and application as Bruton’s tyrosine kinase inhibitor. The claimed pyrimidine derivative is shown in structure I (R = H, Cl, F, or trifluoromethyl; R1 = H, Cl or F; M = amido group). The claimed compound is prepared via multiple steps (procedure given). The prepared compound can inhibiting Bruton’s tyrosine kinase, can be used for treating Burkitt’s lymphoma, mantle cell lymphoma, diffuse 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).Safety of N-(3-Aminophenyl)acrylamide

The Article related to pyrimidine derivative preparation brutons tyrosine kinase inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Safety of N-(3-Aminophenyl)acrylamide

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

On February 22, 2017, Ma, Xiaodong; Yu, Haiqing; Song, Anran; Ge, Yang; Song, Zhendong; Huang, Shanshan; Wang, Changyuan; Liu, Kexin published a patent.SDS of cas: 16230-24-3 The title of the patent was Preparation of purine compounds as BTK tyrosine kinase inhibitors for treating large B cell lymphoma, follicular lymphoma or chronic lymphocytic leukemia. And the patent contained the following:

The invention relates to purine compounds, isomers or pharmaceutically acceptable salts or hydrates with formula of I, wherein R1 is one of H, methoxy, Me, chloro or fluoro; R2 is morpholine, 1-methylpiperazine, 1-ethylpiperazine, etc. The invention compounds can be used for treating diseases caused by BTK tyrosine kinase, especially disseminated anaplastic 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).SDS of cas: 16230-24-3

The Article related to purine preparation btk tyrosine kinase inhibitor lymphoma leukemia, 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 September 28, 2018, Zhai, Xin; Zhou, Yuhong; Gong, Ping; Jing, Tongfei; Lei, Hongrui; Guo, Ming; Xing, Lingyun published a patent.Electric Literature of 16230-24-3 The title of the patent was Tetrahydropyrido[4,3-d]pyrimidine derivative useful in treatment of ATX and EGFR related diseases and its preparation. And the patent contained the following:

The invention relates to tetrahydropyrido[4,3-d]pyrimidine derivative of formula I useful in treatment of ATX and EGFR related diseases and its preparation Compounds I, wherein L is O(CH2)m, S(CH2)m, NH(CH2) m, etc.; m is 0-4; P is O, S, NH, etc; R1 is C6-10 aryl or 5-10-membered heteroaryl (containing 1-3 heteroatoms selected from N, O and S); R3 is C1-6 alkyl, C2-6 alkenyl, C3-6 alkenyl amino, C6-10 aryl, etc.; their optical stereoisomers, pharmaceutically acceptable salts, solvates, or prodrug, are claimed. The inventive compound shows high inhibitory activity on ATX and EGFR, and can be applied in the drugs for preventing and/or treating the diseases caused by abnormal expression of ATX and EGFR, especially the drugs for preventing and/or treating fibrosis and cancer. 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 tetrahydropyrido pyrimidine preparation treatment atx egfr disease, 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 December 1, 2011, Yang, Shengyong; Wei, Yuquan published a patent.Recommanded Product: 16230-24-3 The title of the patent was (Arylamino)purine derivatives as EGFR and VEGFR inhibitors and their preparation, pharmaceutical compositions and use in the treatment of cancer. And the patent contained the following:

(Arylamino)purine derivatives of formula I and their preparation methods are disclosed. The derivatives of formula I have inhibitory effects on non-small cell lung cancer with deletion mutation of exon 19 or L858R point mutation of exon 21 in epidermal growth factor receptor (EGFR) and vascular endothelial growth factor receptor (VEGFR). Compounds of formula I wherein R1 is H, C0-4 alkyl, C3-7 cycloalkyl, C3-7 cycloalkyl-C1-8 alkyl, C1-8 alkyl-C3-7 cycloalkyl, 3- to 8-membered heterocycloalkyl, 3- to 8-membered heterocycloalkylamino and 6- to 8-membered (hetero)aryl; R2 is H, NH2, OH, F, Cl, Br, CF3, C1-8 alkyl, C1-8 alkoxy, C1-8 alkylamino, 6- to 12-membered aryloxy and 6- to 12-membered arylamino; R3 is C3-7 cycloalkyl, C1-8 alkyl-C3-7 cycloalkyl and 6- to 80-membered (hetero)aryl; R4-R8 are independently H, F, Cl, Br, CF3, C1-8 alkoxy, C0-4 dioxaalkylene, (1-methyl-4-piperidinyl)aminocarbonyl, (1-methyl-4-piperazinyl)aminocarbonyl, etc.; are claimed. Example compound I (R1 = Pr-i, R2 = R5 = R6 = R7 = R8 = H, R3 = 4-bromphenyl and R4 = 4-methyl-1-piperazinyl) was prepared via cyclocondensation of 5-amino-4-(isopropylamino)-2-[4-(4-methylpiperazin-1-yl)phenyl]aminopyrimidine with 4-bromophenyl isothiocyanate. All the invention compounds were evaluated for their EGFR and VEGFR inhibitory activity. From the assay, it was determined that example compound I exhibited the IC50 values of 0.001 and 0.004 μM against RGFR-L858R and VEGFR2, resp. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Recommanded Product: 16230-24-3

The Article related to arylamino purine preparation egfr vegfr inhibitor treatment cancer, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Recommanded Product: 16230-24-3

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

On March 16, 2016, Lu, Xianping; Yu, Jindi; Yang, Qianjiao; Li, Zhibin; Pan, Desi; Shan, Song; Zhu, Jiangfei; Wang, Xianghui; Liu, Xiangheng; Ning, Zhiqiang published a patent.Safety of N-(3-Aminophenyl)acrylamide The title of the patent was Preparation of pyrimidine derivatives and their application as the inhibitor of JAK. And the patent contained the following:

The invention is related to the preparation of pyrimidine derivatives I and their application as the inhibitor of JAK. The invention compounds I, wherein X is halogen; R1 is H, cyano, halogen, etc.; R2 is H or halo; R3 is C1-6 alkyl or substituted alkyl; n is integer of 1-7; p is integer of 1-3; A is C6-10 aryl or C5-10 heteroaryl; and their pharmaceutically acceptable salts are claimed. Compound I was prepared by multi-step procedure (procedure given). The pyrimidine derivatives I or pharmaceutically acceptable salts have JAK kinase inhibitory activity, especially have selectivity and high inhibitory activity on JAK3 kinase, and can be used for preparing JAK3 kinase inhibitors as well as medicines for prevention or treatment of diseases related to JAK3 kinase activity abnormity, so as to prevent or treat diseases related to JAK3 kinase activity abnormity. From assay, it was determined that I exhibited the IC50 value of 0.65-1.22 uM against JAK1. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Safety of N-(3-Aminophenyl)acrylamide

The Article related to preparation pyrimidine derivative application inhibitor jak, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Safety of N-(3-Aminophenyl)acrylamide

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

On July 27, 2018, Zhang, Yinsheng; Ren, Jing; Gao, Yong; Zhao, Damin; Zhou, Yu; Wang, Qinglin published a patent.Reference of N-(3-Aminophenyl)acrylamide The title of the patent was Bruton’s tyrosine kinase (BTK) inhibitor for preparing drugs for preventing or treating BTK-mediated diseases. And the patent contained the following:

The inhibitor has the structural formula I, wherein R1 includes hydrogen, halogen, etc.; R2 includes hydrogen, hydroxyl, etc., L includes imino, oxygen, etc.. The inhibitor includes N-(3-((2-((1-hydroxy-1,3-dihydrobenzo[c][1,2]oxaborol-6-yl)amino)-5-(trifluoromethyl)pyrimidin-4-yl)amino)phenyl)acrylamide, N-(3-((2-((2-hydroxy-2,3-dihydrobenzo[d][1,2]oxaborol-6-yl)amino)-5-(trifluoromethyl)pyrimidin-4-yl)amino)phenyl)acrylamide, etc., or its pharmaceutically acceptable salts. A pharmaceutical composition comprises the inhibitor and its pharmaceutically acceptable salts, and is used in preparing drugs for preventing or treating BTK-mediated diseases. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Reference of N-(3-Aminophenyl)acrylamide

The Article related to acrylamide preparation bruton tyrosine kinase inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Reference of N-(3-Aminophenyl)acrylamide

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

On April 13, 2016, Lu, Xianping; Yu, Jindi; Yang, Qianjiao; Li, Zhibin; Pan, Desi; Shan, Song; Zhu, Jiangfei; Wang, Xianghui; Liu, Xiangheng; Ning, Zhiqiang published a patent.HPLC of Formula: 16230-24-3 The title of the patent was Preparation of pyrimidine derivatives as JAK inhibitors. And the patent contained the following:

The title pyrimidine derivatives shown in formula I [wherein, R1 is H, halogen, etc.; R2 is H, hydroxy, carboxyl, etc.; R3 is selected from H, halogen, cyano, etc.; R4 is H, C1-6 alkyl, etc.; X is NH or O] or pharmaceutically acceptable salts thereof were prepared as JAK inhibitors, and especially showed selective high inhibitory activity on JAK3. For example, compound II was prepared in a multi-step synthesis. The title pyrimidine derivatives can be used in preparing the drugs for preventing and treating the diseases related to JAK3 activity abnormality, e.g., autoimmune diseases, inflammation, cancer, proliferative diseases, bone resorption disease, organ transplant rejection, rheumatoid arthritis, Crohn’s disease, systemic lupus erythematosus, multiple sclerosis, type I diabetes, psoriasis, allergic diseases, asthma, chronic obstructive pulmonary disease, leukemia or lymphoma. (assay data given). 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 preparation pyrimidine derivative human jak 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 August 13, 2015, Zhang, Dawei published a patent.Application of 16230-24-3 The title of the patent was Substituted pyrimidines useful as EGFR-T790M kinase inhibitors and their preparation. And the patent contained the following:

The invention is directed to pyrimidines of formula I, their derivatives, pharmaceutically acceptable salts, solvates and hydrates thereof. The compounds and compositions of the invention have protein kinases inhibitory activities and are expected to be useful for the treatment of protein kinases and/or mutants mediated diseases and conditions. Compounds of formula I wherein R1 is H, C1-6 alkoxy, F, Cl and CF3; R2 is C1-6 alkyl and acyl; with provisions; and pharmaceutically acceptable salts, solvates, prodrugs, stereoisomers, tautomers and metabolites thereof, are claimed. Example compound II was prepared by amination of 2,4-dichloro-5-(trifluoromethyl)pyrimidine with 1-(4-(4-aminophenyl)piperazin-1-yl)ethanone; the resulting 1-[4-[4-[[4-chloro-5-(trifluoromethyl)pyrimidin-2-yl]amino]phenyl]piperazin-1-yl]ethanone underwent amination with N-(3-aminophenyl) prop-2-enamide to give compound II. The invention compounds were evaluated for their EGFR-T790M kinase inhibitory activity. From the assay, it was determined that compound II exhibited Kd value of 0.54 nM. 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 preparation egfr t790m kinase 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