专利号:US-5204456-A 优先权日:1986-04-08 标题:Derivatives of nucleosides and their use for the synthesis of oligonucleotides 发明人:MOLKO DIDIER; SCHULHOF JEAN-CLAUDE; TEOULE ROBERT 权利人:COMMISSARIAT ENERGIE ATOMIQUE 摘要:The invention relates to derivatives of nucleosides and their use for the synthesis of oligonucleotides. These derivatives are in accordance with the formula: (I) in which B represents a radical derived from guanine, cytosine or adenine, whose exocylic NH group is protected by the group with R1 representing a hydrogen atom or a alkyl radical and R2 a hydrogen atom, and alkyl radical, an alkoxy radical and optionally substituted aryloxy radical, R3 represents a hydrogen atom, the dimethoxytrityl radical or the radical R4 represents a hydrogen atom, the radical of formula: or a radical suitable for the synthesis of polynucelotides and R5 represents a hydrogen atom or the protected or unprotected hydroxyl OH radical.
专利号:US-6951932-B2 优先权日:2001-10-25 标 题:Synthesis of 2-aralkoxyadenosines and 2-alkoxyadenosines 发明人:MOORMAN ALLAN R 权利人:KING PHARMACEUTICALS RES & DEV 摘要:The invention provides new methods for synthesis of 2-aralkyloxyadenosines and 2-alkoxyadenosines. The invention is particularly useful for synthesis of 2-[2-(4-chlorophenyl)ethoxy]adenosine. Preferred methods of the invention include activating a guanosine compound followed by hydrolysis; alkylating the hydrolyzed compound with subsequent animation to provide a 2-aralkyloxyadenosine or a 2-alkoxyadenosine compound.
专利号:US-5300638-A 优先权日:1991-07-31 标题:Asymmetric synthesis of taxol side chain 发明人:FARINA VITTORIO; HAUCK SHEILA I 权利人:BRISTOL MYERS SQUIBB CO 摘要:The present invention relates to a process for the preparation of (3R, 4S)-3-hydroxy-4-phenyl-2-azetidinone derivatives which are useful intermediates in the synthesis of taxol from baccatin III, said process comprises reacting an acyloxyacetyl halide with an imine derived from L-threonine; and to compounds of formula (III) which are produced in said process: ##STR1## wherein Ar is phenyl; R 1 is hydrogen, an acyl radical of a carboxylic acid, or a carbonic acid ester radical; R 2 is hydrogen or a carboxy protecting group; and R 3 is hydrogen or a hydroxy protecting group.
专利号:US-2009306400-A1 优先权日:2006-03-27 标 题:Convergent process for the synthesis of taxane derivatives. 发明人:HENRI JOHN T; MCCHESNEY JAMES D; VENKATARAMAN SYLESH K; LAMB RODGER L; FOSTER JONATHAN E; SUMNER CHRISTIAN M; YE SHANGPING 权利人:HENRI JOHN T; MCCHESNEY JAMES D; VENKATARAMAN SYLESH K; LAMB RODGER L; FOSTER JONATHAN E; SUMNER CHRISTIAN M; YE SHANGPING 摘要:The present invention is broadly directed to novel compounds useful for the synthesis of biologically active compounds, including taxane derivatives, and convergent processes for the preparation of these taxane derivatives and their intermediates.
专利号:US-4264775-A 优先权日:1976-10-27 标 题:Synthesis of β-aminostyrenes 发明人:WHITE WILLIAM A 权利人:LILLY CO ELI 摘要:A simple process for the preparation of beta -aminostyrenes proceeds from anilines by successively diazotizing, reacting with a vinyl ester, and reacting with a secondary amine without purification of the intermediate products. The compounds are reactive enamines useful in organic synthesis.
专利号:US-4369312-A 优先权日:1980-07-04 标 题:Method of producing oxo-containing azetidinone compounds 发明人:HASHIMOTO MASASHI; ARATANI MATSUHIKO; HAGIWARA DAIJIRO; SAWADA KOZO; ONAMI TETSUO 权利人:FUJISAWA PHARMACEUTICAL CO 摘要:This invention relates to a novel method of producing oxo-containing azetidinone compounds, or salts thereof, or hydrates thereof, said compounds having utility as antimicrobial agents and as intermediates for the synthesis of other azetidinone compounds having antimicrobial activity.