Tetracyclic analogues of Camptothecin Preparation procedures, Intermediates used in the preparation of these Intermediates, procedures,Use of the tetracyclic analogues for the preparation of Drugs and medicines and Pharmaceutical compositions.

摘要

2. The purpose of the application is to formulate a form response (I) formula similar to campotecina, racemized, corresponding or any combination. R1 represents a lower radical tar, lower calcium, lower asphalt, lower haloalkyl, lower dioxyl alkyl or lower aspha R2, R3 and R4 represent a kind of radical h, hydroxy, low oxygen, arilalcoxi, halogenation, halogenation, hydrogen halide, fluorosulfonyl fluoride, lower tar, sulphurous acid, cyanogen, lower cyanofluor, nitro, nitroso formate, imine, lower amidaryl (CH2) mr6r7, CH2, mor6, CH2, mnr6c (or) R8, (CH2) MC (R8), respectively,O (CH2) mnr6r7, OC (o) nr6r7, OC (o) (CH2) mco2r6, arilo or arilalq uilo were replaced (i.e., replaced 1 to 4 times in arilo group) or not, and the substitute was lower tar, halogen, nitro, amino, lower halogen, lower hydroxide or lower alcox R3 or R3, R4 or R4 and R5 independently form a chain of 3 or 4 links, in which the elements in the chain are selected from the CH, CH2, O, s, n or nr9 groups; R5 represents a radical h, halogen, lower haloalkyl group, lower tar, low oxygen, low tar, lower diene dioxide and lower alkyl group.cycloalkyl, cycloalkylalkyl, cyano, cyano alkyl, alkanesulfonylalkyl, lower hydroxyalkyl, nitro (CH2) mC (O) R8, (CH2) mNR6C (O) R8, (CH2) mNR6R7, (CH2) mN (CH3) (CH2 ) nNR6R7, (CH2) mOC (O) R8, (CH2) NOC (O) NR6R7, aryl or lower arylalkyl substituted (i.e. one to four times in the aryl group) or non-substituted, where the substituent is a lower alkyl. , halogen, nitro, amino, lower alkylamino, halogenoalkyl lower, hydroxyalkyl lower, lower alkoxy or lower alkoxyalkyl; R6 and R7 independently represent H, a lower alkyl, hydroxyalkyl lower, lower alkylaminoalkyl, lower aminoalkyl, cycloalkyl radical,Low cyclopentyl glycol, low cyclopentyl glycol, low oxygen alkyl, low halogen glycol or arilo or