and kinetically competent catalysts for this transformation. The fleeting transmetalation intermediate has been successfully synthesized through an alternative synthetic organometallic pathway at lower temperature, allowing for in situ NMR study of the C–N bond reductive elimination step. This study addresses key factors governing the mechanism of the nickel-catalyzed Buchwald–Hartwig amination process
Processes and compounds for the preparation of substituted naphthylindole derivatives
申请人:Dragan A. Vladimir
公开号:US20060183917A1
公开(公告)日:2006-08-17
The present invention provides processes for the preparation of substituted naphthylindole derivatives that can be used as inhibitors of plasminogen activator inhibitor-1(PAI-1). In certain embodiments of the invention, the processes involve reactions that include one or more of an Oppenauer oxidation, a Fischer indole synthesis, a methyl ether cleavage, or coupling a substituted methyltetrazole with a substituted naphthol.
PROCESSES AND COMPOUNDS FOR THE PREPARATION OF SUBSTITUTED NAPHTHYLINDOLE DERIVATIVES
申请人:DRAGAN A. Vladimir
公开号:US20080071091A1
公开(公告)日:2008-03-20
The present invention provides processes for the preparation of substituted naphthylindole derivatives that can be used as inhibitors of plasminogen activator inhibitor-1 (PAI-1). In certain embodiments of the invention, the processes involve reactions that include one or more of an Oppenauer oxidation, a Fischer indole synthesis, a methyl ether cleavage, or coupling a substituted methyltetrazole with a substituted naphthol.
PROCESS FOR PRODUCING 2-($g(v)-ALKOXYCARBONYLALKANOYL)-4-BUTANOLIDE AND LONG-CHAIN $g(v)-HYDROXY CARBOXYLIC ACID
申请人:TORAY INDUSTRIES, INC.
公开号:EP0794182A1
公开(公告)日:1997-09-10
2-(ω-alkoxycarbonyl alkanoyl)-4-butanolide can be produced unexpectedly with a high selectivity and yield through condensation reaction of γ-butyrolactone with a highly available, loω-price dicarboxylate as represented by the following general formula:
ROOC(CH2)nCOOR
(where n denotes an integer of 7-13, and R denotes an alkyl group or an alkenyl group). Furthermore, a long-chain ω-hydroxycarboxylic acid can be produced by subjecting 2-(ω-alkoxycarbonyl alkanoyl)-4-butanolide to hydrolysis and decarboxylation and reducing the carbonyl groups in the resultant product into methylene groups.
通过γ-丁内酯与以下通式所代表的高可得性、低ω价二羧酸盐的缩合反应,可以意外地以高选择性和高产率生产出 2-(ω-烷氧羰基烷酰基)-4-丁内酯:
ROOC(CH2)nCOOR
(其中 n 表示 7-13 的整数,R 表示烷基或烯基)。此外,将 2-(ω-烷氧羰基烷酰基)-4-丁内酯进行水解和脱羧反应,并将所得产物中的羰基还原成亚甲基,可制得长链ω-羟基羧酸。
Conversion of 7-methoxy-3,4-dihydro-2H-1-benzopyran-2-one into the corresponding dimethyl ortho ester
作者:David G. Bourke、David J. Collins
DOI:10.1016/s0040-4020(97)00007-0
日期:1997.3
7-Methoxy-3,4-dihydro-2H-1-benzopyran-2-one 2 was converted into 3-(2'-tert-butyldimethylsilyloxy-4'-methoxyphenyl)-N-Methyl-N-phenylpropanamide 25 and reaction of this with methyl trifluoromethanesulfonate, followed by reaction with sodium methoxide, gave 2,2,7-trimethoxy-2H-1-benzopyran 1a in 55% overall yield from 25. A similar methylation/methoxide sequence using 3-(2'-benzyloxy-4'-methoxyphenyl)-N-methyl-N-phenylpropanamide 18 gave a mixture which contained trimethyl 3-(2'-benzyloxy-4'-methoxyphenyl)orthopropanoate 20a and reaction of this mixture with a solution of sodium in tert-butanol gave a product in which 2,2,7-trimethoxy-2H-1-benzopyran 1a was detected, but not isolable. (C) 1997 Elsevier Science Ltd.