Patent ID: 6670345
Filing Date: 2003-12-30
Classification: C07J

Abstract:
A betulinic acid derivative of formula 2 wherein R, R1, R2, R3, R4, R5, R6 and R7 independently or in combination represent the following groups: R is H; R1 is H, Br, Cl, F or I; R2 is H and R3 is OCOC(CH3)3, OCO(CH2)mX (where m is 2 to 7 and X is H, Cl, Br, or F), OCOCH2C6HnY (where n is 2 to 4), OCOC10HsY, OCOCH2C10HsY (where s is 2 to 6) (where Y is H, Cl, Br, F, I, CN, NO2, NH2, CF3, OH, OCH3, OC2H5, CHCl2 or CmH2m+1 (where m is 1 to 7)), OCOC6HnZa (where n is 2 to 4 and Za is CN, NO2, NH2, OH, OCH3, OC2H5, CHCl2 or CmH2m+1 (where m is 1 to 7)); OCOC6H2Zb (where Zb is Cl, Br, F, I, CN, NO2, NH2, CF3, OH, OCH3, OC2H6, CHCl2 or CmH2m+1 (where m is 1 to 7)) OCOC6HqY (where q is 0 or 1 and Y is H, Cl, Br, F, I, CN, NO2, NH2, CF3, OH, OCH3, OC2H6, CHCl2 or CmH2m+1 (where m is 1 to 7)), OCO(CH2)uNH2 (where u is 1 to 8), OCOC6H4COOH, OCOC6Hw(COOH)L (where w is 2 or 3, and L is H, Cl, Br, F, NO2 or NH2), OCOCHQQ1, (where Q is H, CH3 or Ph and Q1 is OH, Cl, Br or OCOCH3), OCOCH&boxH;C(Xâ€²)2 (where Xâ€² is H, CH3 or C2H5), Oâ€”COâ€”C(Br)&boxH;CHCOOH, â€ƒâ€”OOCCH(OH)CH(Ph)A (where A is NH2, or NHC6HnZâ€² (where n is 2 to 4 and Zâ€² is H, Cl, F or Br)), R7 is O and R4 is OM (where M is Na+, K+, Li+), OB (where B is H, CH3, C2H5, C3H7, or C4H9), O(CH2)tCODâ€² (where t is 1 to 3 and Dâ€² is OH, OCH3, OC2H5, Cl, CN, N3, NH2), OCH2CH2OEâ€² (where Eâ€² is H, CH3, C2H5, or COCH3), OCOCH&boxH;C(Xâ€²)2 (where Xâ€² is H, CH3 or C2H5), OCO(CH2)xZâ€² (where x is 1 to 16 and Zâ€² is H, Cl, F or Br), OCOC6HqFâ€² (where q is 0 to 4), OCOCH2C6HnFâ€² (where n is 2 to 4) (Fâ€² is H, Cl, Br, F, I, CN, NO2, CF3, CHCl2, OH, OCH3, OC2H5 or CmH2m+1 (where m is 1 to 7)), OCH2CHO, OCH2CH&boxH;NOGâ€², OCH2CH2NHOGâ€² (where Gâ€² is H, CH3, SO2C6H4CH3, OCOCH3, OCOC6H5, phenyl or benzyl substituted derivatives), OCH2CH&boxH;NNHC6HnY, OCH2CH2NHNHC6HnY (where n is 2 to 4), OCH2CH&boxH;NNHC10HsY (where s is 2 to 6), OCH2CH2CH2NHNHC10HmY (where Y is H, Cl, Br, F, I, CN, CF3, CHCl2, NO2, NH2, OH, OCH3, OC2H5 or CmH2m+1 (where m is 1 to 7)), OCH2CH2N(Hâ€²)2 (where Hâ€² is H, CH3, C2H5, C3H7, C4H9, C6H5, C6H5CH2 or its substituted derivative wherein the substituent is selected from Cl, Br, CN, F, I, NO2, NH2, CF3, CHCl2, OH, OCH3, OC2H5 or CmH2m+1 (where m is 1 to 7)), O-(3deoxybetulinic acid), O-(3-deoxydihydrobetulinic acid), or O-(2-Bromo-3-oxo-28-oyl-lupane); R5 is H or Br; R6 is CH3, or CH2Br.