CAS: 475058-41-4; (S)-3-Hydroxypiperidine Hydrochloride

相似化合物

24211-55-0 64051-79-2 143900-43-0

上下游产品

CAS号62367-59-3 (3S)-1-甲基哌啶-3-醇

(S)-1-叔丁氧羰基-3-羟基哌啶置于盐酸体系中,用 1,4-二氧六环,水,乙酸乙酯 作为反应溶剂,化学反应 2.0H,反应生成 (S)-3-羟基哌啶 盐酸盐
参考文献:一种工业化生产(S)-3-(4-溴苯基)哌啶的方法
标题:一种工业化生产(S)-3-(4-溴苯基)哌啶的方法
摘要:本发明属于化学医药合成领域,提供了一种可以工业化生产(S)‑3‑(4‑溴苯基)哌啶的方法.该方法以(S)‑1‑叔丁氧羰基‑3‑羟基哌啶为起始原料,通过脱叔丁氧羰基保护基得到(S)‑3‑羟基哌啶盐酸盐a;中间体a和二氯亚砜缩合反应生成五元环亚磺酸酯中间体b;中间体b氧化后反应生成五元环磺酸酯c;然后化合物c和芳基负离子发生亲核取代反应,同时构型翻转,反应生成目标产物(S)‑3‑(4‑溴苯基)哌啶.整个工艺没有用到高压氢化,重氮化等操作,也没有使用手性拆分试剂,总体成本较低,操作简便,能保持较高的手性纯度,适合工业化大生产.

专利信息

专利号:US-2019040070-A1
优先权日:2016-02-09
标 题:Process for the synthesis of stable amorphous ibrutinib
发明人：MAIER THOMAS; KARAPETYAN INNA; ARAKELYAN ALVARD; MARGARYAN TAMARA; SARGSYAN VARDAN; STEPANYAN HEGHINE; ABOVYAN HERMINE; GERBER AESCHBACHER ROMAN; HAFERKAMP SVEN
权利人:AZAD PHARMACEUTICAL INGREDIENTS AG
摘要:Disclosed herein is a new route of synthesis and a new stable amorphous form of ibrutinib. Also disclosed are pharmaceutical compositions, oral dosage forms and the use of the amorphous ibrutinib in the treatment of mantle cell lymphoma or chronic lymphocytic leukemia.

专利号:US-9676783-B2
优先权日:2008-10-22
标 题:Method of treatment using substituted pyrazolo[1,5-A] pyrimidine compounds
发明人：HAAS JULIA; ANDREWS STEVEN W; JIANG YUTONG; ZHANG GAN
权利人:ARRAY BIOPHARMA INC
摘要:Compounds useful in the synthesis of compounds for treating pain, cancer, inflammation, neurodegenerative disease or Typanosoma cruzi infection in a mammal.

专利号:DK-2725028-T3
优先权日:2008-10-22
标题:Substituted pyrazolo [1,5-a] pyrimidine compounds as intermediates in the synthesis of kinase inhibitors TRK

专利号:EP-2725028-A1
优先权日:2008-10-22
标题 :Substituted pyrazolo[1,5-]pyrimidine compounds as intermediates in the synthesis of TRK kinase inhibitors

专利号:EP-2725028-B1
优先权日:2008-10-22
标题 :Substituted pyrazolo[1,5-]pyrimidine compounds as intermediates in the synthesis of TRK kinase inhibitors

专利号:HU-E030413-T2
优先权日:2008-10-22
标 题:Substituted pyrazolo[1,5-]pyrimidine compounds as intermediates in the synthesis of TRK kinase inhibitors