Fischer Indolization and Its Related Compounds. VIII. Formation of 4-Aminoindole Derivatives on the Fischer Indolization of 2-Methoxyphenylhydrazone Derivatives

Ishii, H; Murakami, Y; Takeda, H; Furuse, T

HERO ID

4933265

Reference Type

Journal Article

Year

1974

HERO ID 4933265
In Press No
Year 1974
Title Fischer Indolization and Its Related Compounds. VIII. Formation of 4-Aminoindole Derivatives on the Fischer Indolization of 2-Methoxyphenylhydrazone Derivatives
Authors Ishii, H; Murakami, Y; Takeda, H; Furuse, T
Journal Chemical and Pharmaceutical Bulletin
Volume 22
Issue 9 (1974)
Page Numbers 1981
Abstract   Fischer indolization of ethyl pyruvate 5-chloro-2-methoxyphenylhydrazone (6) with anhydrous zinc chloride gave ethyl 4-amino-6-chloroindole-2-carboxylate (12) as a main product, with three other expected in doles, (7), (8) and (5). Cyclization of ethyl pyruvate 2-methoxyphenylhydrazone (1) with p-toluenesulfonic acid in the presence of diethyl malonate afforded ethyl 4-(ethoxycarbonylacetamido)-indole-2-carboxylate (28) and diethyl 4-(ethoxycarbonylacetamido)-3, 6'-biindole-2, 2'-dicarboxylate (30) with five other indole derivatives, (11), (10), (26), (27), and (32). The pathway leading to such a 4-aminoindole product in the abnormal Fischer indolization of a 2-methoxyphenylhydrazone derivative is discussed.
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