专利号:US-2004106815-A1 优先权日:2002-12-02 标题 :Selective synthesis of organophosphites
专利号:US-2012172336-A2 优先权日:2009-03-19 标 题:Fosfluconazole Derivatives, Synthesis, and Use in Long Acting Formulations 发明人:GONNISSEN YVES; VOORSPOELS JODY 权利人:GONNISSEN YVES; VOORSPOELS JODY; SEPS PHARMA N V 摘要:The invention relates to a compound of formula (1) and the salts, N-oxides, quaternary amines, and stereoisomers thereof, wherein R 1 to R 2 are as defined in the claims. The invention further relates to intermediates and methods for the preparation of the compounds of formula (I). The invention also relates to the compounds of formula (I) for use as a medicament, particularly for the prevention or treatment of fungal infections.
专利号:US-4537714-A 优先权日:1982-07-20 标 题 :Process for the preparation of lower alkyl esters of N-L-α-aspartyl-L-phenylalanine and of new intermediates for their preparation 发明人:MUELLER HANS-RUDOLF; BOLLINGER HEINRICH 权利人:EPROVA AG 摘要:The invention relates to a selective process for the preparation of N-L-α-aspartyl-L-phenylalanine-1-lower alkyl ester which comprises: n A. reacting an L-aspartic acid 4-arylmethyl ester with a n (i) 1,3-diketone; or n (ii) acylacetic ester; n in the presence of a base to form the salt of n (i') L-N-(1-alkyl-2-acyl-vinyl)-aspartic acid 4-arylmethyl ester; or n (ii') L-N-(1-alkyl-2-alkoxycarbonyl-vinyl)-aspartic acid 4-arylmethyl ester, n and then either: n (1) reacting salt (i') or (ii') with an organic or inorganic acid halide having the formula X-A, wherein X represents a halogen and A has the meaning indicated hereinafter, or with an acid anhydride to form ##STR1## wherein R represents an alkyl radical with 1 to 6 carbon atoms; n R' represents an alkyl or alkoxy radical with 1 to 6 carbon atoms; n Ar represents the phenyl, nitrophenyl, halogenphenyl or alkylphenyl radical; and n A represents an acyl with 2 to 12 carbon atoms, alkoxycarbonyl with 2 to 12 carbon atoms, or a phosphoric acid, phosphorous acid, sulfuric acid, sulfurous acid or sulfonic acid radical; n and reacting ester (I) with an L-phenylalanine lower alkyl ester; or n (2) reacting a salt of (i') or (ii') with a phosphorazo-L-phenyl lower alkyl ester; to form n (i') N-L-α-N'-(1-alkyl-2-acyl-vinyl)-aspartyl-L-phenylalanine-1-lower alkyl-4-arylmethyl ester; or n (ii') N-L-α-N'-(1-alkyl-2-alkoxycarbonyl)aspartyl-L-phenylalanine-1-lower alkyl-4-arylmethyl ester; n B. reacting (i') or (ii') with a strong acid to split off the respective N-(1-alkyl-2-acyl-vinyl) or N-(1-alkyl-2-alkoxycarbonyl-vinyl) protective group and produce: n (iii) N-L-α-aspartyl-L-phenylalanine-1-lower alkyl-4-(arylmethyl)ester; and n C. subjecting ester (iii) to catalytic hydrogenation to selectively split off the 4-(arylmethyl)-ester group and leave the N-L-α-aspartyl-L-phenylalanine-1-lower alkyl ester product. n Novel intermediates for the synthesis are also disclosed.
专利号:EP-1567468-B1 优先权日:2002-12-02 标题:A selective synthesis of organophosphites
专利号:RU-2164229-C2 优先权日:1994-10-19 标 题 :Antiviral substrate isoster esters of aspartate protease or their salts, method of their synthesis, pharmaceutical preparation and composition
摘要:Zefirov, N. S.; Matveeva, E. D.; Shuvalov, M. V., Science of Synthesis: Multicomponent Reactions, (2013) 1, 280. 摘要:Stankevič, M.; Włodarczyk, A., Science of Synthesis: Knowledge Updates, (2024) 1, 424.