Method for the formation of intermediate compounds hemisintesis structures and derivatives and related compounds and ecteinascidina tetrahidroisoquinolinfenoles and intermediaries In This method Application

摘要

This invention relates to compounds of the formula: ##STR00001## wherein: the substituent groups defined by R.sub.1, R.sub.2 are each independently selected of H, C(.dbd.O)R', C.sub.1 C.sub.18 alkyl, C.sub.2 C.sub.18 alkenyl, C.sub.2 C.sub.18 alkynyl, or aryl; each of the R' groups is independently selected from the group consisting of H; OH; NO.sub.2; NH.sub.2; SH; CN; halogen; .dbd.O; C(.dbd.O)H; C(.dbd.O)CH.sub.3; CO.sub.2H; or C.sub.1 C.sub.18 alkyl, C.sub.2 C.sub.18 alkenyl, C.sub.2 C.sub.18 alkynyl, or aryl, each of which, independently, may be substituted with one or more substituents selected from the group consisting of halogen, cyano, hydroxy, nitro, azido; alkanoyl, carboxamido, alkyl, alkenyl, alkynyl, aryloxy, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, aminoalkyl, carbocylic aryl having 6 or more carbons, and aralkyl; X.sub.2 is OX.sub.1 or N(X.sub.1).sub.2 wherein each X.sub.1 is independently H, C(.dbd.O)R' where R' is as defined, C.sub.1 C.sub.18 alkyl, C.sub.2 C.sub.18 alkenyl, C.sub.2 C.sub.18 alkynyl, aryl, alkoxy, heterocyclyl, or two X.sub.1 groups together form a cyclic substituent on the nitrogen atom, or X.sub.1 is SO.sub.2CH.sub.3 when X.sub.2 is OX.sub.1, or N(X.sub.1).sub.2 is NHCOalkylCOOH, NHBiotin, NH(aa).sub.y where aa is amino acid acyl and Y is 1, 2 or 3 optionally with a amide terminal group, protected NHCOCH(NH.sub.2)CH.sub.2SH, NHCOalkenylaryl substituted with CF.sub.3, or m-methoxycarbonylbenzoylNH; wherein N(X.sub.1).sub.2 is not NH.sub.2; X.sub.3 is selected of OR.sub.1 where R.sub.1 is as defined, CN, (.dbd.O), or H; X.sub.4 is--H or C.sub.1 C.sub.18 alkyl; and X.sub.5 is selected of H, or R.sub.1 where R.sub.1 is as defined; provided that the compound is not ecteinascidin 583 or 597, which are useful for treating tumors.