合成路线:The esterification of proline (I) with SOCl2 and ethanol gives ethyl prolinate (II),which by treatment with NH3 in methanol is converted into prolinamide (III).The acylation of (III) with cyclopropylcarbonyl chloride (IV) by means of K2CO3 in acetone yields 1-cyclopropylcarbonyl-2-carbamoylpyrrolidine (V),which is reduced with LiAlH4 in ether to afford 1-cyclopropylmethyl-2-aminomethylpyrrolidine (VI) (1,2).Finally this compound is condensed with ethyl 5-sulfamoyl-2-methoxybenzoate (VII) by heating at 120 C
参考文献标题:
文献作者:Kaplan,J.P.; et al.(Synthelabo,S.A.)
参考来源:BE 857544; DE 2735036; FR 2360572; FR 2372157; FR 2395261; GB 1555890; JP 7825563; NL 7708571; ZA 7704743
合成路线:The esterification of proline (I) with SOCl2 and ethanol gives ethyl prolinate (II),which by treatment with NH3 in methanol is converted into prolinamide (III).The acylation of (III) with cyclopropylcarbonyl chloride (IV) by means of K2CO3 in acetone yields 1-cyclopropylcarbonyl-2-carbamoylpyrrolidine (V),which is reduced with LiAlH4 in ether to afford 1-cyclopropylmethyl-2-aminomethylpyrrolidine (VI) (1,2).Finally this compound is condensed with ethyl 5-sulfamoyl-2-methoxybenzoate (VII) by heating at 120 C
参考文献标题:
文献作者:(Synthelabo,S.A.)
参考来源:BE 861866; FR 2394529; GB 1560019; JP 7905969; NL 7713631; ZA 7706950
合成路线:The esterification of proline (I) with SOCl2 and ethanol gives ethyl prolinate (II),which by treatment with NH3 in methanol is converted into prolinamide (III).The acylation of (III) with cyclopropylcarbonyl chloride (IV) by means of K2CO3 in acetone yields 1-cyclopropylcarbonyl-2-carbamoylpyrrolidine (V),which is reduced with LiAlH4 in ether to afford 1-cyclopropylmethyl-2-aminomethylpyrrolidine (VI) (1,2).Finally this compound is condensed with ethyl 5-sulfamoyl-2-methoxybenzoate (VII) by heating at 120 C
参考文献标题:
文献作者:Obitz,D.C.L.(Synthelabo,S.A.)
参考来源:FR 2393794
合成路线:The esterification of proline (I) with SOCl2 and ethanol gives ethyl prolinate (II),which by treatment with NH3 in methanol is converted into prolinamide (III).The acylation of (III) with cyclopropylcarbonyl chloride (IV) by means of K2CO3 in acetone yields 1-cyclopropylcarbonyl-2-carbamoylpyrrolidine (V),which is reduced with LiAlH4 in ether to afford 1-cyclopropylmethyl-2-aminomethylpyrrolidine (VI) (1,2).Finally this compound is condensed with ethyl 5-sulfamoyl-2-methoxybenzoate (VII) by heating at 120 C
参考文献标题:
文献作者:Kaplan,J.P.; et al.(Synthelabo,S.A.)
参考来源:BE 836752; CA 1039731; CH 612668; DE 2556457; FR 2294698; FR 2327771; FR 2331345; GB 1508880; JP 7748661; NL 7514620; US 4021567; US 4156060; US 4172143; US 4189495; ZA 7507828
产品链接: CAS No. 68475-40-1››