专利号:US-8436206-B2 优先权日:2007-08-03 标 题:Process for the synthesis of (7-methoxy-1-naphthyl) acetonitrile and application in the synthesis of agomelatine 发明人:DUBUFFET THIERRY; LECOUVE JEAN-PIERRE; HERMET JEAN-PAUL 权利人:DUBUFFET THIERRY; LECOUVE JEAN-PIERRE; HERMET JEAN-PAUL; SERVIER LAB 摘要:Process for the industrial synthesis of the compound of formula (I) n nApplication of such process in the synthesis of agomelatine.
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-5072040-A 优先权日:1989-04-06 标 题:Process for synthesis of sulfonylimides 发明人:ARMAND MICHEL 权利人:CENTRE NAT RECH SCIENT; HYDRO QUEBEC 摘要:The invention relates to a process for the synthesis of sulfonylimides. n The process for the synthesis of sulfonylimides of the general formula M[RSO 2 ) 2 N] y , in which M represents a metal chosen from alkali metals, alkaline earth metals, rare earths, Al, Sc, Y and Th, R represents a monovalent radical chosen from linear or branched aliphatic radicals having 1 to 8 carbon atoms, alicyclic radicals having 3 to 8 carbon atoms, aryl radicals having 3 to 8 carbon atoms, and y is a number equal to the valence of M, is characterized in that an ionic nitride of the formula M 3 N y , in which M and y have the meaning given above, is reacted with a sulfonyl halide of the formula RSO 2 X, in which R has the meaning given above, and X is chosen from F or Cl, in an aprotic polar solvent.
专利号:US-4384998-A 优先权日:1981-03-30 标题:Synthesis of thienamycin from D-glucose 发明人:DURETTE PHILIPPE L 权利人:MERCK & CO INC 摘要:Disclosed is a chiral, total synthesis of thienamycin from D-glucose which proceeds via intermediates I, II and III to known aldehyde IV which is known to be useful in the total synthesis of thienamycin (V): ##STR1## wherein: R is lower alkyl having 1-6 carbon atoms or bi-valent alkyl having 2-6 carbon atoms which joins the two sulfur atoms; R 1 is lower alkyl or aralkyl, such as benzyl and the like; and R 2 is hydrogen or a removable protecting group, such as triorganosilyl wherein the organo groups are independently selected from lower alkyl, phenyl and phenylloweralkyl.
专利号:US-4448976-A 优先权日:1981-03-30 标题 :Chiral synthesis of thienamycin from D-gluocose 发明人:DURETTE PHILIPPE L 权利人:MERCK & CO INC 摘要:Disclosed is a chiral, total synthesis of thienamycin from D-glucose which proceeds via intermediates I, II and III to known aldehyde IV which is known to be useful in the total synthesis of thienamycin (V): ##STR1## wherein: R is lower alkyl having 1-6 carbon atoms or bi-valent alkyl having 2-6 carbon atoms which joins the two sulfur atoms; R 1 is lower alkyl or aralkyl, such as benzyl and the like; and R 2 is hydrogen or a removable protecting group, such as triorganosilyl wherein the organo groups are independently selected from lower alkyl, phenyl and phenylloweralkyl.
专利号:US-6399820-B2 优先权日:1998-11-04 标题:Process and reagent useful for the synthesis of sulphanilide which is perhalogenated on the carbon borne by the sulphur atom of the sulphanilide function 发明人:DESMURS JEAN-ROGER; MILLET ANDRE; PEVERE VIRGINIE 权利人:RHODIA CHIMIE SA 摘要:The present invention relates to a process and a reagent useful for the synthesis of sulphanilide which is perhalogenated on the carbon borne by the sulphur atom of the sulphanilide function. This persulphonylation process is characterized in that it comprises a step of placing a nucleophile, whose nucleophilic atom is a nitrogen, in contact with a reagent comprising, for successive or simultaneous addition, a heavy halide of sulphonyl, advantageously sulphonyl chloride, and an organic base comprising a trivalent atom from column V whose lone pair is conjugated directly or indirectly to a bond, and in that the organic part of the said sulphonyl is perhalogenated, advantageously perfluorinated, on the carbon borne by the sulphur. Application to the synthesis of intermediates for organic chemistry.