CAS: 87600-98-4; 4,6-Dichloro-5-Pyrimidinecarboxylic Acid

相似化合物

5305-40-8 5305-45-3 87600-72-4

上下游产品

2,6-dichloro-pyrimidine carbaldehyde 4,6-dichloropyrimidine-5-carboxylic acid chloride 4,6-dichloro-5-pyrimidinecarboxylic acid methyl ester N-(2-(tert-butyldimethylsilyloxy)ethyl)-4,6-dichloro-N-(7-(cyclopropanecarboxamido)-1-(2-methoxyphenyl)-1H-indol-5-yl)pyrimidine-5-carboxamide 4,6-dichloro-N-(7-(cyclopropanecarboxamido)-1-(2-methoxyphenyl)-1H-indol-5-yl)-N-(2-hydroxyethyl)pyrimidine-5-carboxamide

4,6-二氯-5-嘧啶甲醛置于sodium Chlorite,Sodium Dihydrogenphosphate,2-甲基-2-丁烯体系中,用 水,叔丁醇 作为反应溶剂,化学反应 4.0H,以59%的收率获得产物4,6-二氯-5-嘧啶羧酸
参考文献:新型2,4,6-三取代-5-嘧啶羧酸作为过氧化物酶体增殖物激活的受体γ(pparγ)部分激动剂的设计,合成和结构活性关系研究,具有与罗格列酮相当的抗糖尿病功效
标题:新型2,4,6-三取代-5-嘧啶羧酸作为过氧化物酶体增殖物激活的受体γ(pparγ)部分激动剂的设计,合成和结构活性关系研究,具有与罗格列酮相当的抗糖尿病功效
摘要:设计和合成了一系列新颖的2,4,6-三取代嘧啶-5-羧酸衍生物,目的是生产抗糖尿病药的过氧化物酶体增殖物激活受体γ(pparγ)部分激动剂.药效团驱动的内部筛选方法可鉴定出化合物7,从而鉴定出具有2,4,6-三取代嘧啶-5-羧酸核的化合物9.9的构效关系研究确定了4,6-双苄硫基-2-甲基硫基嘧啶-5-羧酸(50)是所有筛选化合物中最有吸引力的.x射线共晶结构为50Pparγ上的键揭示了与激活功能2(af-2)位点无关的关键氢键相互作用与完全激动剂的氢键相互作用不同.化合物50在pparγ-Gal4功能试验中显示出典型的pparγ部分激动剂特性,并且与罗格列酮相比在3T3-L1细胞中的脂肪细胞分化更弱.此外,尽管有50种药效比罗格列酮弱10倍,但在db / Db小鼠中有50种与罗格列酮具有相当的抗糖尿病功效.
DOI:10.1021/jm100443S

专利信息

专利号:US-2017327504-A1
优先权日:2014-10-30
标 题:Synthesis of Substituted 1H-Pyrazolo[3,4-D]Pyrimidines
发明人：ROSE CHRISTOPHER; SILBERGER HERBERT; SCHREINER ERWIN; FELZMANN WOLFGANG; MARAS NENAD
权利人:SANDOZ AG
摘要:The present invention refers to the synthesis and intermediates of substituted bicyclic compounds by using a central 1H-pyrazolo[3,4-d]pyrimidine of formula (I), which is assembled starting from 4,6-dichloropyrimidine carboxylic acid. The invention in particular refers to the synthesis of the Bruton's tyrosine kinase (Btk) inhibitor 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one(ibrutinib) and its synthesis intermediates.

专利号:WO-2014074883-A1
优先权日:2012-11-08
标题 :Novel synthesis of ld101
发明人：THOMPSON ANDREW S; CHENG HUA
权利人:LYNDOR BIOSCIENCES L L C
摘要:Novel synthetic methods for preparation of LD101, a compound according to formula (A) are disclosed.

专利号:CA-2965558-A1
优先权日:2014-10-30
标题 :Synthesis of substituted 1h-pyrazolo[3,4-d]pyrimidines

专利号:EP-3212624-A1
优先权日:2014-10-30
标 题 :Synthesis of substituted 1h-pyrazolo[3,4-d]pyrimidines

专利号:CN-106795124-A
优先权日:2014-10-30
标题 :Synthesis of Substituted 1H-pyrazolo[3,4-d]pyrimidines

专利号:WO-2016066673-A1
优先权日:2014-10-30
标 题 :Synthesis of substituted 1h-pyrazolo[3,4-d]pyrimidines