CAS: 186550-13-0; 1-Boc-3-Aminopyrrolidine

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103831-11-4 114715-38-7 114715-39-8

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1-Boc-吡咯烷-3-甲酸置于palladium On Activated Charcoal 二苯基磷酸,氢气,三乙胺体系中,用 甲醇,甲苯 用作溶剂,化学反应 20.0H,反应生成3-氨基吡咯烷-1-羧酸叔丁酯
参考文献:新型非肽氰胺类化合物,可有效和可逆地抑制人组织蛋白酶k和l.
标题:新型非肽氰胺类化合物,可有效和可逆地抑制人组织蛋白酶k和l.
摘要:鉴定出含有1-氰基吡咯烷基环的化合物是组织蛋白酶k和l的有效抑制剂和可逆抑制剂.原始的铅化合物1抑制组织蛋白酶k和l的ic(50)值分别为0. 37和0.45M.通过取代喹啉部分的化合物1的修饰导致了n-(1-氰基-3-吡咯烷基)苯磺酰胺的合成(2).发现化合物2是组织蛋白酶k和l的有效抑制剂,组织蛋白酶k的k(i)值为50 Nm.用1-氰基氮杂环丁烷取代化合物2的1-氰基吡咯烷使抑制剂的效力提高了10-折.效力的增加可能是由于该化合物对酶活性位点的硫醇盐的化学反应性增强.当在ph 7的谷胱甘肽存在下进行测定时,证明了这一点.0有利于gsh硫醇盐阴离子的形成.在这些测定条件下,由于在gsh硫醇盐和1-氰基氮杂环丁烷抑制剂之间形成了无活性的复合物,因此1-氰基氮杂环丁烷系列的效能丧失.1-氰基吡咯烷基抑制剂表现出时间依赖性抑制作用,这使我们能够确定与人组织蛋白酶k的缔合和解离速率常数.获得
Doi:10.1021/jm0003440

专利信息

专利号:US-9551018-B2
优先权日:2006-02-13
标 题 :Process for the preparation of optically active chiral amines
发明人：ROBINS KAREN; SCHEUER UWE; HOHNE MATTHIAS
权利人:LONZA AG
摘要:The present invention relates to the production of optically pure secondary amines, which can be used as intermediate products in a synthesis of for instance pharmaceutical products.

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-8030501-B2
优先权日:2006-07-28
标题 :Process for producing optically active 3-amino nitrogen-containing compounds
发明人：OHNUKI MASATOSHI; IZUMIDA MASASHI; NISHIYAMA AKIRA; MATSUMOTO SHINGO
权利人:KANEKA CORP
摘要:Aiming at production of an optically active 3-amino nitrogen-containing compound which is useful as an intermediate in synthesis of medicines and pesticides, in particular, an optically active 1-protected-3-aminopyrrolidine derivative, from an inexpensive and readily available raw material by a process which is efficient and can be practiced industrially, an optically active 3-amino nitrogen-containing compound is produced by performing a reaction of an optically active 3-substituted nitrogen-containing compound with ammonia, methylamine, ethylamine or dimethylamine in the presence of water. In addition, a 1-protected-3-aminopyrrolidine derivative is produced by performing a reaction of an optically active 1-protected-3-(sulfonyloxy)pyrrolidine derivative with ammonia, methylamine, ethylamine, or dimethylamine in the presence of methanol, ethanol, n-propanol, or isopropanol under a pressure of less than 30 barr.

专利号:US-9833457-B2
优先权日:2008-01-25
标题:Tricyclic compounds as modulators of TNF-α synthesis and as PDE4 inhibitors
发明人：MJALLI ADNAN M M; GADDAM BAPU; POLISETTI DHARMA RAO; KOSTURA MATTHEW J; GUZEL MUSTAFA
权利人:VTV THERAPEUTICS LLC
摘要:The present invention relates to chemical compounds of Formula (I) are as herein defined, pharmaceutical compositions, and methods of use in the treatment of conditions or disorders mediated by TNF-α or by PDE4, including but not limited to psoriatic arthritis.

专利号:US-8003785-B2
优先权日:2008-06-18
标 题 :Halo-substituted pyrimidodiazepines
发明人：CAI JIANPING; CHEN SHAOQING; CHU XIN-JIE; LUK KIN-CHUN; MISCHKE STEVEN GREGORY; SUN HONGMAO; WOVKULICH PETER MICHAEL
权利人:TAKEDA PHARMACEUTICAL
摘要:The present invention provides PLK1 inhibitor compounds of formula I: n nuseful in the treatment or control of cell proliferative disorders, particularly oncological disorders. These compounds and formulations containing such compounds may be useful in the treatment or control of solid tumors, such as, for example, breast, colon, lung and prostate tumors and other oncological diseases such as non-Hodgkin's lymphomas. Also provided are intermediate compounds useful in the synthesis of compounds of formula I.

专利号:US-9708336-B2
优先权日:2014-01-22
标题 :Metallo-beta-lactamase inhibitors
发明人：MANDAL MIHIR; TANG HAIFENG; XIAO LI; SU JING; LI GUOQING; YANG SHU-WEI; PAN WEIDONG; TANG HAIQUN; DEJESUS REYNALDA; HICKS JACQUELINE; LOMBARDO MATTHEW; CHU HONG; HAGMANN WILLIAM; PASTERNAK ALEX; GU XIN; JIANG JINLONG; DONG SHUZHI; DING FA-XIANG; LONDON CLARE; BISWAS DIPSHIKHA; YOUNG KATHERINE; HUNTER DAVID N; ZHAO ZHIQIANG; YANG DEXI
权利人:MERCK SHARP & DOHME
摘要:The present invention relates to compounds of formula (I) that are metallo-β-lactamase inhibitors, the synthesis of such compounds, and the use of such compounds for use with β-lactam antibiotics for overcoming resistance.