CAS: 6154-30-9; 2,5-Dibromo-4-Nitro-1H-Imidazole

相似化合物

6963-65-1 65902-59-2 18874-52-7

上下游产品

CAS号65902-59-2 2-溴-4-硝基咪唑 | CAS号162759-90-2 2,4-二溴-1-甲基-5-硝...

4-硝基-3H-咪唑置于溴,碳酸氢钠体系中,用 水 作为反应溶剂,化学反应 10.0H,以88%的收率获得产物2,5-二溴-4-硝基咪唑
参考文献:硝基咪唑并唑类药物,Delamanid 和相关化合物的简明顺序合成
标题:硝基咪唑并唑类药物,Delamanid 和相关化合物的简明顺序合成
摘要:已经开发了一种简洁,无保护基团和顺序的路线,用于合成基于硝基咪唑的 Fda 批准的耐多药抗结核药物 Delamanid 和抗利什曼原虫先导候选药物 Vl-2098.该合成需要手性环氧化物(11和17)作为关键中间体.手性环氧化物11通过顺序反应级联即合成.,烯丙基化,选择性n-芳基化,Mitsunobu醚化,Sharpless不对称二羟基化和环氧化,不需要任何特殊/干燥的反应条件.环氧化物合成所涉及的步骤在克规模上也很有效.环氧化物11合成后,通过与2-溴-4-硝基咪唑12反应实现delamanid的合成,总收率为27%.同样,抗利什曼原虫先导候选药物 Vl-2098 也以 36% 的总产率合成.
DOI:10.1039/d0Ra01662D

专利信息

专利号:US-8129544-B2
优先权日:2002-10-15
标题:1-substituted-4-nitroimidazole compound and method for preparing the same
发明人：GOTO FUMITAKA; TAKEMURA NORIAKI; OTANI TADAAKI; HASEGAWA TAKESHI; TSUBOUCHI HIDETSUGU; UTSUMI NAOTO; FUJITA SHIGEKAZU; KURODA HIDEAKI; SHITSUTA TAKUYA; SASAKI HIROFUMI
权利人:GOTO FUMITAKA; TAKEMURA NORIAKI; OTANI TADAAKI; HASEGAWA TAKESHI; TSUBOUCHI HIDETSUGU; UTSUMI NAOTO; FUJITA SHIGEKAZU; KURODA HIDEAKI; SHITSUTA TAKUYA; SASAKI HIROFUMI; OTSUKA PHARMA CO LTD
摘要:The present invention relates to a 1-substituted-4-nitroimidazole compound represented by the general formula (1) or a salt thereof, n n(wherein R is a hydrogen atom, a lower alkoxy group-substituted lower alkyl group, a phenyl-lower alkoxy group-substituted lower alkyl group, a cyano-substituted lower alkyl group, a phenyl-lower alkyl group which may have lower alkoxy groups as the substituents in the phenyl ring or a group of the formula —CH 2 R A ; X is a halogen atom or a group of the formula —S(O)n-R 1 ) and method for preparing the same. The compound of the formula (1) is a useful compound as an intermediate for synthesis of various pharmaceutical and agricultural chemicals, particularly, as intermediates for antitubercular agents.

专利号:CN-105439957-B
优先权日:2015-11-24
标 题:A kind of method of the bromo- 4- nitroimidazoles of synthesis 2-