CAS: 143900-44-1; (S)-Tert-Butyl 3-Hydroxypiperidine-1-Carboxylate

上下游产品

vinyl acetate N-tert-butoxycarbonyl-3-piperidinol tert-butyl dicarbonatedi-tert-butyl dicarbonate (S)-3-hydroxypiperidine hydr°Chloride (S)-3-methanesulfonyloxy-piperidine-1-carboxylic acid tert-butyl ester (S)-N-methylpiperidin-3-yl butyrate (3R)‐4‐amino‐3‐(4-phenoxyphenyl)‐1‐(1‐tert-butoxycarbonylpiperidine-3-yl)-1H-pyrazolo[3,4-d]pyrimidine tert-butyl (+)-(3S)-3-(benzyloxy)piperidine carbamate

3-吡啶磺酸置于rh/c,氢气,三乙胺,Sodium Hydroxide体系中,用 甲醇,乙醇,水 用作溶剂,20.0~210.0 °C,4.3 Mpa 条件下,反应 48.3H,反应生成(S)-1-叔丁氧羰基-3-羟基哌啶
参考文献:一种(S)-1-叔丁氧羰基-3-羟基哌啶的制备方法
标题:一种(S)-1-叔丁氧羰基-3-羟基哌啶的制备方法
摘要:本发明公开了一种(S)‑1‑叔丁氧羰基‑3‑羟基哌啶的制备方法,涉及生物制药技术领域,包括如下步骤,步骤一,制备3‑羟基吡啶(2)作为原料;步骤二,通过3‑羟基吡啶(2)制备消旋3‑羟基哌啶(3);步骤三,消旋3‑羟基哌啶(3)经d‑酒石酸制得衍生物(2S,3S)‑n‑(4‑氯苯基)‑2,3‑二羟基丁酰胺酸(4);步骤四,将d‑酒石酸制得衍生物(2S,3S)‑n‑(4‑氯苯基)‑2,3‑二羟基丁酰胺酸(4)拆分得(S)‑羟基哌啶盐(5);步骤五,将混合物进行萃取,浓缩,结晶,制得(S)‑1‑叔丁氧羰基‑3‑羟基哌啶盐(5),本发明制备工艺减少了合成步骤,同时提高收率,可利用回收手性拆分剂,适合工业化生产.

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-2018282336-A1
优先权日:2014-10-30
标题:Active Acrylamides
发明人：FELZMANN WOLFGANG; BRUNNER STEFANIE; LENGAUER HANNES
权利人:SANDOZ AG
摘要:The present invention refers to the synthesis and intermediates of substituted bicyclic compounds, which are used as a masked form of acrylamides and 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-2017137446-A1
优先权日:2016-02-09
标题:Process for the synthesis of stable amorphous ibrutinib

专利号:EP-3414248-A1
优先权日:2016-02-09
标题 :Process for the synthesis of stable amorphous ibrutinib

专利号:US-2018222909-A1
优先权日:2015-07-29
标 题 :Process for the preparation of ibrutinib and new synthesis intermediate
发明人：BERTOLINI GIORGIO; FERRANDO ILARIA; SADA MARA
权利人:OLON SPA
摘要:Subject-matter of the invention is a process for the preparation of ibrutinib and intermediate compound.

专利号:CN-113816962-A
优先权日:2015-01-14
标题 :Synthesis of Bruton's tyrosine kinase inhibitors