【药物名称】Clotiazepam, Y-6047, Distensan, Rizen, Rize
化学结构式(Chemical Structure):
参考文献No.803955
标题:Clotiazepan
作者:Casta馿r, J.; Chartterjee, S.S.
来源:Drugs Fut 1976,1(8),363
合成路线图解说明:

By cyclocondensation of 2-methylamino-3-(o-chlorobenzoyl)-5-ethylthiophene (I) with ethyl glycinate hydrochloride (A) in pyridine.

合成路线图解说明:

By cyclization of 2-(N-methyl-2-aminoacetamido)-3-(o-chlorophenyl)-5-ethylthiophene (II) in pyridine - benzol - acetic acid. The starting thiophene (II) can also be obtained in two different ways both starting from the 2-methylamino-3-(o-chlorobenzoyl)-5-ethylthiophene (I): (a) The thiophene (I) is condensed with chloroacetyl chloride giving 2-(N-methylchloroacetamido)-3-(o-chlorobenzoyl)-5-ethylthiophene (III), which by treatment with NaI gives the corresponding iodoacetamido derivative (IV). This compound reacts with NaN3 giving the corresponding azide (V), which finally reacts with HBr affording the thiophene (II). (b) The reaction of the thiophene (I) with N-carbobenzoxyglycyl chloride gives the carbobenzoxy derivative (VI) which is then hydrolyzed with HBr to give (II).

参考文献No.900188
标题:
作者:Nakanishi, M.; et al. (Yoshitomi Pharmaceutical Industries Ltd.)
来源:DE 2107356
合成路线图解说明:

By cyclocondensation of 2-methylamino-3-(o-chlorobenzoyl)-5-ethylthiophene (I) with ethyl glycinate hydrochloride (A) in pyridine.

合成路线图解说明:

By cyclization of 2-(N-methyl-2-aminoacetamido)-3-(o-chlorophenyl)-5-ethylthiophene (II) in pyridine - benzol - acetic acid. The starting thiophene (II) can also be obtained in two different ways both starting from the 2-methylamino-3-(o-chlorobenzoyl)-5-ethylthiophene (I): (a) The thiophene (I) is condensed with chloroacetyl chloride giving 2-(N-methylchloroacetamido)-3-(o-chlorobenzoyl)-5-ethylthiophene (III), which by treatment with NaI gives the corresponding iodoacetamido derivative (IV). This compound reacts with NaN3 giving the corresponding azide (V), which finally reacts with HBr affording the thiophene (II). (b) The reaction of the thiophene (I) with N-carbobenzoxyglycyl chloride gives the carbobenzoxy derivative (VI) which is then hydrolyzed with HBr to give (II).

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