PRODUCTION OF 1-DEOXYPACLITAXEL

摘要

PROBLEM TO BE SOLVED: To obtain a new compound useful as an antitumor agent. SOLUTION: This 1-deoxypaclitaxel is a compound of formula I R is H, a 1-6 alkyl, a 2-6C alkyl, a 2-6C alkynyl, a 3-7-membered ring containing a heterocyclic ring, etc.; RA, RB are each H, HNC(O)R, etc.; RC, RD are each H, hydroxy, fluoro, etc.; R<2> is RX, RY, etc., [RX is an alkyl, an alkenyl, etc.; RY is formula II (W is a bond; R , R , R are each H, nitro, cyano, etc.), etc.]; R<4> is an alkyl, an alkenyl, etc.; R<6> , R<6> ' are each H or hydroxyl; R<7> is H, hydroxy, etc.; R<7> ' is H; R<9> , R<9> ' are each H, hydroxy, etc.; R<10> , R<10> ' are each H, hydroxy, etc., R<14> is H or hydroxy; R<19> is methyl, etc., L is O or S} or their salts. As the compound of the formula I, 10-deacetyl-1-deoxy-9- dihydropaclitaxel-7,9-acetonide is cited. The compound of the formula I is obtained by using 1-deoxybaccatin as a starting material and through 6 processes such as a deacetylation, a protection by a protecting group, an esterification and removal of the protecting group, etc.