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Process for preparing piperazic acid and its conversion to acylated bicyclic rings n, that link n, n useful as intermediates for caspase inhibitors.
Process for preparing piperazic acid and its conversion to acylated bicyclic rings n, that link n, n useful as intermediates for caspase inhibitors.
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机译：制备哌嗪酸并将其转化为连接n，n的酰化双环n的方法，n可用作胱天蛋白酶抑制剂的中间体。
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摘要
A process for converting compound G to compound H: ** (Formula) ** in which: R1 is a straight chain alkyl of C2-C4alkyl substituted on the alpha carbon relative to the rest COOH with NO2 or N (R4 ) (R4) and optionally substituted at any carbon with one or more substituents selected from linear or branched C1C6, alkenyl or alkynyl linear or branched C2-C6 linear or branched alkyl or C1C6, O-alkenyl or linear or branched alkynyl of C2-C6, oxo, halo, NO2, N (R4) (R4), CN, Ar or O-Ar; R2 is selected from hydrogen, linear or branched C1-C6 alkyl, linear or branched C2-C6 alkynyl or Ar, wherein said alkyl, alkenyl or alkynyl is optionally substituted with Ar; n is 0 or 1; Ar is a monocyclic or bicyclic structure saturated rings, partially saturated or unsaturated, wherein each ring contains 5 to 7 ring atoms and each ring optionally contains from 1 to 3 heteroatoms selected from O, S Ny; wherein Ar is optionally substituted at one or more ring atoms with one or more substituents independently selected from linear or branched C1-C6 alkyl, or linear or branched alkynyl of C2C6, O-alkyl straight or branched C1-C6 , O-alkenyl or alkynyl linear or branched C2-C6 alkyl, oxo, halo, NO2, N (R4) (R4), CN, or O-Ar1 Ar1; wherein Ar1 is a structure of monocyclic or bicyclic ring saturated, partially saturated or unsaturated, wherein each ring contains 5 to 7 ring atoms and each ring optionally contains from 1 to 3 heteroatoms selected from O, N and S; and each R4 is independently H or an amino protecting group selected, with the proviso that both R4 are not simultaneously hydrogen, said process comprising the steps of: (a) suspending compound G in an organic solvent selected from dichloroethane, dichloromethane , toluene, chlorobenzene, chloroform, monoglyme, diglyme or CCl4; (B) adjust temperature of the resulting solution to between 20 and 100; (C) adding 2 to 4 equivalents of base and more than about 1 equivalent of RSOpClp to said solution, wherein R is absent or selected from linear or branched C1-C6 or Ar alkyl, and each p is independently 1 or 2; and (d) incubating said solution for a period of between 2 and 18 hours.
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