CAS: 188111-79-7; (R)-1-Boc-3-Aminopiperidine

相似化合物

625471-18-3 138060-07-8 168466-84-0

上下游产品

CAS号915226-43-6 (R)-3-氨基甲酰基哌啶-1... | CAS号320580-76-5 (R)-叔-丁基 3-(((苄...

N-叔丁氧羰基-3-哌啶酮置于磷酸吡哆醛,Immobilized Codex® Amine ω-Transaminase,异丙胺体系中,用 二甲基亚砜 用作溶剂,以70%的收率获得(R)-(-)-1-Boc-3-氨基哌啶
参考文献:使用固定的ω-转氨酶不对称合成高附加值手性胺.
标题:使用固定的ω-转氨酶不对称合成高附加值手性胺.
摘要:手性n-杂环分子,尤其是具有氨基官能团的化合物,例如3-氨基哌啶是有价值的中间体,用于生产大量具有药理特性的生物活性化合物.在本文中,通过固定化的ω-转氨酶(tas-Imb),异丙胺作为胺供体和吡ido醛-吡咯烷酮-前手性前体1-Boc-3-哌啶酮的胺化,合成了3-氨基-1-Boc-哌啶的两种对映体.描述了作为辅助因子的5'-磷酸(plp).与其他方法相比,本方法仅需一个步骤即可从商业底物开始以高收率和高对映体过量提供目标化合物.通过使用不同的市售固定化酶进行反应,评估在不同实验条件下的催化活性和对映选择性.分批和半连续系统均重复使用了最有效的酶.所选择的生物催化剂在反应条件下显示出非常好的稳定性,在几个循环后就转化率和对映体过量而言提供了一致的结果.鉴于将这种可持续方法发展到工业规模,报告的结果可能具有实际意义.
Doi:10.3762/bjoc.15.6

专利信息

专利号:US-8178672-B2
优先权日:2004-10-19
标 题:Synthesis of imidazooxazole and imidazothiazole inhibitors of p38 MAP kinase
发明人：ASHWELL MARK A; TANDON MANISH; LAPIERRE JEAN-MARC
权利人:ASHWELL MARK A; TANDON MANISH; LAPIERRE JEAN-MARC; ARQULE INC
摘要:An efficient route for the synthesis is of formula (I) of imidazooxazole and imidazothiazole inhibitors of the p38 MAP kinase pathway, useful as therapeutics for disease conditions including inflammation and auto-immune responses is described.

专利号:US-8728750-B2
优先权日:2006-09-06
标 题 :Process for preparation of optically active N-protected 3-aminopyrrolidine or optically active N-protected 3-aminopiperidine and the corresponding ketones by optical resolution of the racemic amine mixtures employing a bacterial omega-transaminase
发明人：ROBINS KAREN; BORNSCHEUER UWE; HÖHNE MATTHIAS
权利人:ROBINS KAREN; BORNSCHEUER UWE; HÖHNE MATTHIAS; LONZA AG
摘要:The present invention relates to the production of optically active amines, which can be used as intermediate products in a synthesis of for instance pharmaceutical products.

专利号:US-2025101021-A1
优先权日:2022-06-14
标 题:Methods of making tolebrutinib
发明人：BAILLY FRÉDÉRIC; BENELLI CHRISTOPHE; BORIE CYRIL; BOSCH MICHAËL; CABOS CLAUDE; CHARAUDEAU ALEXIS; JANSSENS LAURENCE; PACQUET FRANÇOIS; RODIER FABIEN; SALLÉ LAURENT; SODO ALFRED; VIGNE SYLVIE
权利人:PRINCIPIA BIOPHARMA INC
摘要:Disclosed herein are improved synthetic routes for making (R)-1-(1-acryloylpiperidin-3-yl)-4-amino-3-(4-phenoxyphenyl)-1 H-imidazo[4,5-c]pyridin-2(3H)-one (tolebrutinbib). Also disclosed herein are novel compounds used in the synthesis of of (R)-1-(1-acryloylpiperidin-3-yl)-4-amino-3-(4-phenoxyphenyl)-1 H-imidazo[4,5-c]pyridin-2(3H)-one.

专利号:US-2022363662-A1
优先权日:2021-04-20
标题 :Compounds as lxr agonists
发明人：PUJALA BRAHMAM; SATHE BALAJI DASHRATH; DANODIA ABHINANDAN; GUPTA ASHU; SONI SANJEEV; KUMAR VIVEK; ANSARI AMANTULLAH; KHAN FARHA; SARKAR ARINDAM; PAYGHAN PAVAN V
权利人:INTEGRAL BIOSCIENCES PRIVATED LTD
摘要:The present invention generally discloses compounds having LXR (the liver X receptor) agonistic activity, to the use of such compounds in the treatment of various disorders such as proliferative disorders, Alzheimer's disease, inflammatory diseases, and diseases characterized by defects in cholesterol and lipid metabolism. Specifically, the present invention discloses compound of formula (IA) which exhibit LXR agonist activity, specifically to LXRβ. The invention also discloses method of synthesis of said compounds, method of using said compounds, pharmaceutical compositions comprising said compounds and method of using thereof.

专利号:US-2009111985-A1
优先权日:2004-10-19
标 题 :Synthesis of imidazooxazole and imidazothiazole inhibitors of p38 map kinase

专利号:WO-2023091726-A1
优先权日:2021-11-18
标题:Inhibitors of cyclin‑dependent kinase 12 (cdk12)
发明人：BENOIT GUILLAUME; CARULLI JOHN; CHEN FEI; CHUAQUI CLAUDIO; CIBLAT STEPHANE; COOPER ELLIOT; DAGENAIS ROBIN; HU SHANHU; KABRO ANZHELIKA; LAPLACA DEREK; MARINEAU JASON; MOEBIUS DAVID; MOON DIANE; SOLODININ ANDREI; WHITMORE KENNETH
权利人:SYROS PHARMACEUTICALS INC
摘要:The present invention provides chemical compounds that inhibit one or more families of kinases (e.g., serine/threonine kinases, including one or more of the families of CDK proteins, and in particular, CDK12). More specifically, the present invention provides CDK12 inhibitors, of formula (I), pharmaceutically acceptable salts and isotopically labeled derivatives thereof, pharmaceutical compositions containing the compounds/inhibitors, and methods of their synthesis and use in treating proliferative diseases (e.g., a bladder cancer, a breast cancer, Ewing's sarcoma, a gastric cancer, a gastrointestinal cancer, a hematologic cancer, a lung cancer (e.g., small cell lung cancer (SCLC)), an ovarian cancer (e.g., a high grade serous ovarian cancer), a pancreatic cancer (e.g., pancreatic ductal adenocarcinoma (PDAC)), a brain cancer (e.g., glioblastoma), or a prostate cancer), alone or in combination with a second therapeutic agent. The proliferative disease can be a cancer, benign neoplasm, or pathologic angiogenesis, and any of the therapeutic methods or uses described herein can include a step of diagnosing the patient's disease. In other embodiments of the invention, the compositions described herein (e.g., the compounds, pharmaceutical compositions, and kits containing them) are used for the treatment of myotonic dystrophy (type 1 or type 2).