上下游产品
pyrazinoyl chloride tert-butylaminetert-butylamine (1H-benzo[d][1,2,3]triazol-1-yl)(pyrazin-2-yl)methanone carbon monoxide3-phenylhydroxymethyl-2-N-t-butylpyrazinamide t-butyl (S)-3-(tert-butylcarbamoyl)-piperazine-1-carboxylate (S)-3-tert-Butylcarbamoyl-4-(R)-1-oxiranylmethyl-piperazine-1-carboxylic acid tert-butyl ester [14C]-N-Dealkyl Indinavir 合成工艺路线路线简述
- 合成目标产物 N-T-Butyl Pyrazine Carboxamide 主要起始原料 Tert-Butylamine And Methanone, 1H-Benzotriazol-1-Yl-2-Pyrazinyl-
- (文献来源)合成步骤主要原料 Tert-Butylamine 和 Methanone, 1H-Benzotriazol-1-Yl-2-Pyrazinyl-
📜2-甲酸吡嗪置于草酰氯体系中,化学反应生成2-吡嗪叔丁酰胺
参考文献:手性非外消旋酰胺烯酸酯与(S)-缩水甘油基甲苯磺酸酯的高度非对映选择性反应.口服活性hiv-1蛋白酶抑制剂l-735,524的合成
标题:手性非外消旋酰胺烯酸酯与(S)-缩水甘油基甲苯磺酸酯的高度非对映选择性反应.口服活性hiv-1蛋白酶抑制剂l-735,524的合成
摘要:手性酰胺烯酸酯li-1与(S)-缩水甘油基甲苯磺酸酯11的反应以高非对映体选择性得到环氧化物3,产率为72%.环氧化物3以71%的分离产率转化为口服活性的hiv-1蛋白酶抑制剂l-735,524.
Doi:10.1016/s0040-4039(00)75787-X
专利信息
专利号:US-5612484-A
优先权日:1995-05-18
标题:Process for making HIV protease inhibitors
发明人:ASKIN DAVID; SAGER JESS; ROSSEN KAI; VOLANTE RALPH P; REIDER PAUL J
权利人:MERCK & CO INC
摘要:A process for making a clinically efficacious HIV protease inhibitor Compound J eliminates one step in its synthesis, by an improved, alternative synthesis of the 2(S)-4-picolyl-2-piperazine-t-butyl-carboxamide intermediate.
专利号:DE-69604247-T2
优先权日:1995-07-19
标 题:2-cyanopiperazine and its use for the synthesis of biologically active substances
专利号:EP-0754686-B1
优先权日:1995-07-19
标 题 :2-cyanopiperazine and use thereof for the synthesis of biologically active substances
专利号:EP-0754686-A1
优先权日:1995-07-19
标题 :2-cyanopiperazine and use thereof for the synthesis of biologically active substances
专利号:JP-H10507917-A
优先权日:1994-10-25
标题:Microbial synthesis of HIV protease inhibitors