CAS: 3430-18-0; 2,5-Dibromo-3-Methylpyridine

相似化合物

29232-39-1 61686-65-5 3430-17-9

上下游产品

CAS号3430-21-5 2-氨基-3-甲基-5-溴吡啶 | CAS号1603-40-3 2-氨基-3-甲基吡啶 | CAS号376587-52-9 2-碘-3-甲基-5-溴吡啶 | CAS号878809-70-2 5-溴-2-(4-B°C-哌嗪... | CAS号886365-43-1 5-溴-3-甲基吡啶-2-羧酸 | CAS号65550-78-9 2-溴-5-碘-3-甲基吡啶 | CAS号760207-87-2 5-溴-2-甲氧基-3-甲基吡啶 | CAS号566158-47-2 5-溴-3-甲基-2-(吗啉并)吡啶 | CAS号1003043-34-2 6-溴-5-甲基吡啶-3-硼酸 | CAS号213771-32-5 5-溴-3-甲基-2-吡啶甲酸甲酯 | CAS号156072-86-5 5-溴-3-甲基吡啶-2-甲腈 | CAS号760207-88-3 5-溴-2-异丙氧基-3-甲基吡啶

2-氨基-3-甲基-5-溴吡啶置于氢溴酸,溴,Sodium Nitrite体系中,用 水 用作溶剂,化学反应 4.0H,反应生成2,5-二溴-3-甲基吡啶
参考文献:吡啶酮-氨基衍生物作为mnk1 / 2抑制剂的设计,合成和生物学评估.
标题:吡啶酮-氨基衍生物作为mnk1 / 2抑制剂的设计,合成和生物学评估.
摘要:真核翻译起始因子4E(eif4E)的过度磷酸化在mrna翻译失调和肿瘤细胞信号激活中起主要作用.Eif4E仅被ser209上的促分裂原活化蛋白激酶相互作用的激酶1和2(mnk1 / 2)磷酸化.因此,Mnk1 / 2抑制剂可以降低p-Eif4E的水平并调节肿瘤相关的信号通路.合成了一系列吡啶酮-氨基衍生物,并作为mnk1 / 2抑制剂进行了评估.几种化合物对mnk1 / 2表现出极大的抑制活性,某些化合物对血液癌细胞系表现出中度至优异的抗增殖能力.特别地,化合物42I(mnk1 Ic50 = 7.0 Nm; Mnk2 Ic50 = 6.1 Nm)被证明是针对tmd-8细胞系最有效的化合物,Ic50值为0.91μm.此外,42I可以阻断ct-26细胞系中eif4E的磷酸化水平,42I可以显着抑制ct-26同种异体移植模型的肿瘤生长.这些结果表明,化合物42I是有效治疗结肠癌的有希望的mnk1
Doi:10.1016/j.Bmc.2019.02.007

专利信息

专利号:US-6635767-B2
优先权日:2000-05-23
标 题 :Synthesis of heteroarylamine intermediate compounds
发明人：SONG JINHUA J; YEE NATHAN K; KAPADIA SURESH R
权利人:BOEHRINGER INGELHEIM PHARMA
摘要:Disclosed are novel 2-(5-halopyridyl) and 2-(5-halopyrimidinyl) magnesium halides, processes of making and their use in the efficient synthesis in their respective 5-halo-2-substituted pyridines and pyrimidines.

专利号:US-6822093-B2
优先权日:2000-05-23
标题 :Synthesis of heteroarylamine intermediate compounds
发明人：SONG JINHUA J; YEE NATHAN K
权利人:BOEHRINGER INGELHEIM PHARMA
摘要:Disclosed are novel 2-(5-halopyridyl) and 2-(5-halopyrimidinyl) magnesium halides, processes of making and their use in the efficient synthesis in their respective 5-halo-2-substituted pyridines and pyrimidines.

专利号:US-5760232-A
优先权日:1997-06-16
标题:Synthesis of intermediates useful in preparing bromo-substituted tricyclic compounds
发明人：CHEN XING; POIRIER MARC; WONG YEE-SHING; WU GUANG-ZHONG
权利人:SCHERING CORP
摘要:The invention relates to a process for preparing a compound of the formula ##STR1## comprising: (a) reacting 2,5-dibromo-3-methylpyridine with an amine of the formula NHR 5 R 6 to obtain an amide; n (b) reacting the amide with a compound of formula 3 ##STR2## in the presence of a strong base to obtain a compound of formula 4 ##STR3## (c) converting a compound of formula 4 to the corresponding cyano compound or aldehyde; n (d) reacting the cyano compound or aldehyde with a piperidine derivative to obtain an aldehyde or alcohol of formula 7a or 7b, respectively: ##STR4## (e) cyclizing a compound of formula 7a or 7b; wherein R 1 -R 7 are as defined in the specification.

专利号:US-5998620-A
优先权日:1997-03-25
标 题 :Synthesis of intermediates useful in preparing tricyclic compounds
发明人：CHEN XING; POIRIER MARC; WONG YEE-SHING; WU GUANG-ZHONG
权利人:SCHERING CORP
摘要:The invention relates to a process for preparing a compound of the formula ##STR1## comprising reacting a bromo-substituted pyridine with an amine of the formula NHR 5 R 6 , reacting the resulting amide with an iodo-halomethyl-substituted compound and cyclizing the resultant product, wherein R, R 1 , R 2 , R 3 and R 4 are as defined in the specification; also claimed are a compound of the formula ##STR2## and a process for preparing it from the corresponding halo-substituted benzoic acid.

专利号:US-6495689-B2
优先权日:1998-11-20
标题 :Synthesis of intermediates useful in preparing tricyclic compounds
发明人：BERNARD CHARLES F; CASEY MICHAEL; CHEN FRANK XING; GROGAN DENISE C; POIRIER MARC; WILLIAMS ROBERT P; WONG YEE-SHING; WU GEORGE G
权利人:SCHERING CORP
摘要:Disclosed is a process for preparing a compound having the formula:wherein R, R1, R2, R3, and R4 are independently selected from the group consisting of H, Br, Cl, F, alkyl, or alkoxy.

专利号:EP-0977739-B1
优先权日:1997-03-25
标题 :Synthesis of intermediates useful in preparing tricyclic compounds
发明人：CHEN XING; POIRIER MARC; WONG YEE-SHING; WU GUANG-ZHONG
权利人:SCHERING CORP
摘要:The invention relates to a process for preparing a compound of formula (I), comprising reacting a bromo-substituted pyridine with an amine of the formula NHR5R6, reacting the resulting amide with an iodo-halomethyl-substituted compound and cyclizing the resultant product, wherein R, R?1, R2, R3 and R4¿ are as defined in the specification; also claimed are a compound of formula (a), and a process for preparing it from the corresponding halo-substituted benzoic acid.