Three C-3’-N-sulfonyl and C-7-O-acyl paclitaxel analogues were synthesized from 10-deacetyl baccatinⅢ(10-DAB)and their structures were confirmed by 1H NMR,13C NMR and HR-MS.Among them,the crystal structure of compou...Three C-3’-N-sulfonyl and C-7-O-acyl paclitaxel analogues were synthesized from 10-deacetyl baccatinⅢ(10-DAB)and their structures were confirmed by 1H NMR,13C NMR and HR-MS.Among them,the crystal structure of compound 9 b was determined by single-crystal X-ray diffraction.Compound 9 b crystallizes in monoclinic system,space group P21 with a=12.395(4),b=15.215(5),c=14.905(5)A,β=105.559(4)°and Z=2.In the structure,the introduction of the hydrophobic 3-fluorobenzoyl group at C(7)has little effect on the conformation of tetracyclic system.However,the conformation of the side-chain at C(13)in 9 b is quite different from that of paclitaxel and docetaxel.展开更多
基金supported by the National Natural Science Foundation of China(Nos.21272154 and 81202402)。
文摘Three C-3’-N-sulfonyl and C-7-O-acyl paclitaxel analogues were synthesized from 10-deacetyl baccatinⅢ(10-DAB)and their structures were confirmed by 1H NMR,13C NMR and HR-MS.Among them,the crystal structure of compound 9 b was determined by single-crystal X-ray diffraction.Compound 9 b crystallizes in monoclinic system,space group P21 with a=12.395(4),b=15.215(5),c=14.905(5)A,β=105.559(4)°and Z=2.In the structure,the introduction of the hydrophobic 3-fluorobenzoyl group at C(7)has little effect on the conformation of tetracyclic system.However,the conformation of the side-chain at C(13)in 9 b is quite different from that of paclitaxel and docetaxel.
