专利号:US-5861532-A 优先权日:1997-03-04 标 题:Solid-phase synthesis of N-alkyl amides 发明人:BROWN EDWARD G; NUSS JOHN M 权利人:CHIRON CORP 摘要:Methods for solid phase synthesis of N-alkyl amides comprise reductive amination of carbonyl compounds using a reducing agent and an amine-containing linker bound to a solid support. The methods afford high yields of linker-bound, monoalkylated amines, and subsequent coupling with acid derivatives provide derivatized N-substituted amides in excellent yields after cleavage from the solid-phase. Compositions useful in solid phase synthesis are also described.
专利号:US-6069250-A 优先权日:1995-12-14 标 题 :Method and compositions for the synthesis of dioxolane nucleosides with β-configuration 发明人:MANSOUR TAREK; CIMPOIA ALEX; BEDNARSKI KRZYSZTOF 权利人:IAF BIOCHEM INT 摘要:The present invention relates to methods and compositions for preparing biologically important nucleoside analogues containing 1,3-dioxolane sugar rings. In particular, this invention relates to the stereoselective synthesis of the beta (cis) isomer by glycosylating the base with an intermediate of formula (II) below a temperature of about -10 DEG C. wherein R1 and L are as defined herein.
专利号:US-5919969-A 优先权日:1996-06-05 标 题 :Synthesis of yellow couplers 发明人:CRAWLEY MICHAEL W 权利人:EASTMAN KODAK CO 摘要:The invention provides a method of synthesis of a image-dye forming coupler of formula (I) wherein X is a substituent linked to the coupler by an atom of oxygen, sulfur or nitrogen R1 is an alkyl or aryl group, R2 is a hydrogen atom or an alkyl group; R3 to R7 are the same or different and selected from a hydrogen atom and substituent groups; which method comprises the reaction of a compound of formula (II) wherein R and R1 are the same or different and are as defined above for R1 and X is as defined above with a compound of formula (III) wherein R2 to R7 are as defined above, in the presence of an inert organic solvent.
专利号:US-5698741-A 优先权日:1995-05-25 标题 :Asymmetric synthesis of (-)6-chloro-4-cyclopropyl-ethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one 发明人:THOMPSON ANDREW S; CORLEY EDWARD G; GRABOWSKI EDWARD J J; YASUDA NOBUYOSHI 权利人:MERCK & CO INC 摘要:An improved synthesis of a highly potent HIV reverse transcription inhibitor is disclosed, involving an acetylide and a trifluoromethyl ketone which produces a chiral product in the presence of a chiral amino alcohol.
专利号:US-5663467-A 优先权日:1995-01-23 标题:Synthesis of cyclopropylacetylene 发明人:THOMPSON ANDREW S; CORLEY EDWARD G; HUNTINGTON MARTHA 权利人:MERCK & CO INC 摘要:An improved synthesis of cyclopropylacetylene involving cyclization of 5-halo-1-pentyne in strong base is disclosed, and is useful for preparing compounds with a cyclopropylethynyl substituent, such as an intermediate for a highly potent HIV reverse transcriptase inhibitor or other pharmaceutically active compounds.
专利号:WO-9804535-A1 优先权日:1996-07-26 标 题 :A practical synthesis of benzoxazinones useful as hiv reverse transcriptase inhibitors 发明人:PIERCE MICHAEL ERNEST; RADESCA LILIAN ALICIA 权利人:DU PONT MERCK PHARMA 摘要:The present invention describes novel methods for the synthesis of benzoxazinone compounds which are useful as human immunodeficiency virus (HIV) reverse transcriptase inhibitors. The benzoxazinone of formula (VI-a) is particularly effective in the treatment of HIV.