CAS: 101385-90-4; (S)-1-Benzylpyrrolidin-3-Ol

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101930-07-8 775-15-5 100243-39-8

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1-苄基-吡咯烷置于ferredoxin Reductase,His-Tagged Ferredoxin,His-Tagged P450Pyr Hydroxylase I83H/m305Q/a77S Mutant,β-烟酰胺腺嘌呤二核苷酸,氧气体系中,化学反应 0.08H,反应生成(S)-3-羟基-1-苄基吡咯烷
参考文献:不断发展的p450Pyr羟化酶可在非活化碳原子上实现高度对映选择性的羟化反应.
标题:不断发展的p450Pyr羟化酶可在非活化碳原子上实现高度对映选择性的羟化反应.
摘要:首次证明了单加氧酶的定向进化以实现在非活化碳原子上的羟基化反应具有非常高的对映选择性,其中通过测定酶结构,迭代饱和诱变和高通量筛选获得了p450Pyr羟化酶的三重突变体.基于ms的ee分析,可将n-苄基吡咯烷羟基化为(S)-N-苄基3-羟基吡咯烷的产物ee从53%增加至98%.
Doi:10.1039/c2Cc30779K

专利信息

专利号:US-6566525-B1
优先权日:1998-09-17
标 题:Preparation of N-substituted-hydroxycycloalkylamine derivatives
发明人：KIM SEONG JIN; KIM KEON IL; YANG KYOUNG YOUL
权利人:SAMSUNG FINE CHEMICALS CO LTD
摘要:A process for the preparation of N-substituted-hydroxycycloalkylamine derivatives, that are useful intermediates for the synthesis of various organic chemicals including pharmaceutical and agrochemical compounds, represented by formula (1), by reacting a 1,2-dihydroxalkyl alcohol, represented by the following formula (2), with a thionyl halide to produce an intermediate 1,2-cyclosulfinylalkyl halide represented by the following formula (3); and then cyclizing that intermediate with an amine compounds represented by the following formula (4).In the above structural formuli, * represents an asymmetric carbon atom; R1 is hydrogen or an amino-protecting group; m is an integer of 1-3; and X is halogen. The reactant compounds as well as the compounds made according to this invention have the following substitution pattern:n=1, R2=OH, R3=H and m=1; n=1, R2=H, R3=CH2OH and m=2;n=2, R2=OH, R3=H; and m=2; and n=2, R2=H, R3=CH2OH and m=3.

专利号:WO-2009153649-A1
优先权日:2008-06-19
标 题:Process for preparing 3-substituted pyrrolidine compounds
发明人：SOLDEVILLA MADRID NURIA
权利人:MEDICHEM SA; SOLDEVILLA MADRID NURIA
摘要:Disclosed is a process for preparing 3 -substituted pyrrolidine compounds of formula (VII) or salts thereof, wherein R1 is described herein, which are intermediate compounds useful for the synthesis of darifenacin which is indicated for the treatment of overactive bladder with symptoms of urge, urinary incontinence, and the like, and pharmaceutically acceptable salts thereof. Also disclosed is a process for preparing darifenacin and pharmaceutically acceptable salts 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:EP-1926709-A4
优先权日:2005-08-25
标题:PROCESS FOR THE SYNTHESIS OF A 3-HYDROXYPYRROLIDINE CHIRAL COMPOUND AND DERIVATIVES OF SAID HIGH OPTICAL PURITY COMPOUND

专利号:US-8946422-B2
优先权日:2005-07-27
标题:8-methoxy-9H-isothiazolo[5,4-B]quinoline-3,4-diones and related compounds as anti-infective agents
发明人：BRADBURY BARTON JAMES; WILES JASON ALLAN; WANG QIUPING; HASHIMOTO AKHIRO; LUCIEN EDLAINE; PAIS GODWIN CLARENCE GILROY; DESHPANDE MILIND; PUCCI MICHEAL JOHN; KIM HA YOUNG
权利人:BRADBURY BARTON JAMES; WILES JASON ALLAN; WANG QIUPING; HASHIMOTO AKHIRO; LUCIEN EDLAINE; PAIS GODWIN CLARENCE GILROY; DESHPANDE MILIND; PUCCI MICHEAL JOHN; KIM HA YOUNG; ACHILLION PHARMACEUTICALS INC
摘要:The invention provides compound and salts of Formula I and II, disclosed herein, which includes compounds of Formula A and Formula B: Such compounds possess useful antimicrobial activity. The variables R2, R3, R5, R6, R7, and R9 shown in Formula A and B are defined herein. Certain compounds of Formula I and Formula II disclosed herein are potent and/or selective inhibitors of bacterial DNA synthesis and bacterial replication. The invention also provides antimicrobial compositions, including pharmaceutical compositions, containing one or more compounds of Formula I or Formula II and one or more carriers, excipients, or diluents. Such compositions may contain a compound of Formula I or Formula II as the only active agent or may contain a combination of a compound of Formula I or Formula II and one or more other active agents. The invention also provides methods for treating microbial infections in animals.

专利号:CN-110724084-B
优先权日:2019-11-18
标 题:Synthesis method of (S) -3-hydroxy-1-benzylpyrrolidine