| 摘要 |
The title compds. (I; R=C1-5 alkyl; R1=H, halo, C1-5 alkyl, C1-5 alkoxy; R2=amino, C1-5 alkanoyl, R4NSO2R3;R3=C1-5 alkyl, C2-10 dialkylamino; R4=H, C1-5 alkyl), useful as stomachics and antiemetics, were prepd. Thus, a soln. contg. 1.1g N-(diethylaminoethyl)-5-amino-4-chloro-2-methoxy-benzamide, 815mg Et3N, and 11mL methylene chloride was reacted with 882mg methane sulfonyl chloride in 5mL methylenechloride for 30 min at room temp. to give N-(diethylaminoethyl)-5-bis (methane sulfonyl) amino-4-chloro-2-methoxybenzamide, which was treated with 10% NaOh and 2mL MeOH at 50oC to give 993mg N-(diethylaminoethyl)-4-chloro-5-methane sulfonamido-2-methoxybenzamide.
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