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filingDate 1992-09-16-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 2001-07-24-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber IL-103191-A
titleOfInvention Semisynthesis of the history of Texan using metallic and beta alkoxides, and their intermediates
abstract A process for the preparation of a taxane derivative comprising: providing a metal alkoxide having the bi-, tri-or tetracyclic taxane nucleus, reacting the metal alkoxide with a b-lactam wherein the b-lactam has the formula: wherein R1 is -OR6, -SR7, or -NR8R9; R2 is hydrogen, alkyl, alkenyl, alkynl, aryl, or heteroaryl; R3 and R4 are independently hydrogen, alkyl, alkenyl, alkynyl, aryl, heteroaryl, or acyl, provided, however, that R3 and R4 are not both acyl; R5 is -COR10, -COOR10, -COSR10, -CONR8R10, -SO2R11, or -POR12R13, R6 is hydrogen, alkyl, alkenyl, alkynyl, aryl, heteroaryl, or a hydroxy protecting group, R7 is alkyl, alkenyl, alkynyl, aryl, heteroaryl, or sulfhydryl protecting group, 1598 ד' באב התשס" א - July 24, 2001 R8 is hydrogen, alkyl, alkenyl, alkynyl, aryl, or heteroaryl; R9 is an amino protecting group; R10 is alkyl, alkenyl, alkynyl, aryl, or heteroaryl, R11 is alkyl, alkenyl, aryl, heteroaryl, OR10, or -NR8R14, R12 and R13 are indepdnently alkyl, alkenyl, alkynyl, aryl, heteroaryl, -OR10, or -NR8R14, R14 is hydrogen, alkyl, alkenyl, alkynyl, aryl, or heteroaryl; and converting said intermediate to the taxane derivative. Claimed as novel is the intermediate b-lactam of the formula wherein R1 is -OR6, -SR7, or -NR8R9; R2 is hydrogen, alkyl, alkenyl, alkynyl, aryl, or heteroaryl; R3 and R4 are independently hydrogen, alkyl, alkenyl, alkynyl, aryl, heteroaryl, or acyl, provided, however, that R3 and R4 are not both acyl, and that heteroaryl is other than pyridyl; R5 is -COR10, -COOR10, -COSR10, -CONR8R10, -SO2R11, or -POR12R13, R6 is a hydrogen, alkyl, alkenyl, alkynyl, aryl, heteroaryl, or a hydroxy protecting group, R7 is alkyl, alkenyl, alkynyl, aryl, heteroaryl, or sulfhydryl protecting group, R8 is hydrogen, alkyl, alkenyl, alkynyl, aryl, or heteroaryl; R9 is an amino protecting gorup; R10 is alkyl, alkenyl, alkynyl, aryl, or heteroaryl, R11 is alkyl, alkenyl, alkynyl, aryl, heteroaryl, -OR10, or -NR8R14, R12 and R13 are independently alkyl, alkenyl, alkynyl, aryl, heteroaryl or -NR8R14.
priorityDate 1991-09-23-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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