N-Acetyl-P. m or o-nitro-phenylethylamines and (HCHO). were treated in 60% H,SO./HOAc. via α -amidoalkylation to give 2-acetyl-mono(5, 6, 7 or 8)-nitro-l .2,3.4- tetrahydroisoquinolines. Additionally. solme interesti...N-Acetyl-P. m or o-nitro-phenylethylamines and (HCHO). were treated in 60% H,SO./HOAc. via α -amidoalkylation to give 2-acetyl-mono(5, 6, 7 or 8)-nitro-l .2,3.4- tetrahydroisoquinolines. Additionally. solme interesting phenomena were observed when the comparison between 2-acetyl-5, 6. 7 or 8-nitro-l,2.3.4-tetrahydroisoqui and 2-alkylsulfonyl-5. 6 or 7nitro-l,2.3,4-tetrahydroisoquinolines was made.展开更多
A series of N5-substituted 8-deaza-5,6,7,8-tetrahydromethotrexate derivatives were synthesized and evaluated as inhibitors of dihydrofolate reductase（DHFR）.The results indicated that modification of the pteridine ri...A series of N5-substituted 8-deaza-5,6,7,8-tetrahydromethotrexate derivatives were synthesized and evaluated as inhibitors of dihydrofolate reductase（DHFR）.The results indicated that modification of the pteridine ring of methotrexate（MTX） rendered poor activity against human DHFR.展开更多
基金the new drug discovery foundation of Shanghai instituteof Pharmaceutical Industry and the Analysis Centre of the Second Milita
文摘N-Acetyl-P. m or o-nitro-phenylethylamines and (HCHO). were treated in 60% H,SO./HOAc. via α -amidoalkylation to give 2-acetyl-mono(5, 6, 7 or 8)-nitro-l .2,3.4- tetrahydroisoquinolines. Additionally. solme interesting phenomena were observed when the comparison between 2-acetyl-5, 6. 7 or 8-nitro-l,2.3.4-tetrahydroisoqui and 2-alkylsulfonyl-5. 6 or 7nitro-l,2.3,4-tetrahydroisoquinolines was made.
基金National Natural Science Foundation of China(Grant No.20972011)
文摘A series of N5-substituted 8-deaza-5,6,7,8-tetrahydromethotrexate derivatives were synthesized and evaluated as inhibitors of dihydrofolate reductase（DHFR）.The results indicated that modification of the pteridine ring of methotrexate（MTX） rendered poor activity against human DHFR.
