An Improved Synthesis of Metoclopramide
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概要
- 論文の詳細を見る
This report relates to a new industrial synthesis of metoclopramide (I). Methyl 4-amino-2-methoxybenzoate (V) was prepared by methylation of p-aminosalicylic acid (III) using dimethyl sulfate in the presence of potassium hydroxide in acetone. V and it's saponified product (VI) were chlorinated with iodobenzene dichloride to obtain methyl 4-amino-5-chloro-2-methoxybenzoate (VII) and 4-amino-5-chloro-2-methoxybenzoic acid (VIII) respectively. VIII was also prepared by saponification of VII. VIII was condensed direct with N, N-diethylethylenediamine (IV), of which amino group was activated by phosphorus trichloride, whereby I was obtained in high yields.
- 公益社団法人日本薬学会の論文
- 1971-08-25
著者
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犬飼 紀喜
Central Research Laboratories, Yamanouchi Pharmaceutical Co., Ltd.,
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村上 増雄
Central Research Laboratories, Yamanouchi Pharmaceutical Co., Ltd.
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中野 功二
Central Research Laboratories, Yamanouchi Pharmaceutical Co., Ltd.
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甲田 彰男
Central Research Laboratories, Yamanouchi Pharmaceutical Co., Ltd.
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甲田 彰男
Central Research Laboratories Yamanouchi Pharmaceutical Co. Ltd.
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犬飼 紀喜
Tsukuba Research Laboratories Yamanouchi Pharmaceutical Co. Ltd.
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中野 功二
Central Research Laboratories Yamanouchi Pharmaceutical Co. Ltd.
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