Process for the preparation of (3-cyano-1h-indol-7-yl)...

Details Process for the preparation of (3-cyano-1h-indol-7-yl)... Process for the preparation of (3-cyano-1h-indol-7-yl)...

2007-12-25

2007-12-25

Wilson, James O. (Department: 1624)

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

C548S416000, C548S452000

Reexamination Certificate

active

10466991

ABSTRACT:
The present invention relates to a process for the preparation of (3-cyano-1H-indol-7-yl)[4-(4-fluorophenethyl)piperazin-1-yl]-methanone and salts thereof, characterised in that an indole ester of the formula II in which R is as defined in Claim 1, is converter into 3-cyano-1H-indole-7-carboxylic acid via steps (1) to (4) according to Claim 1, and this is reacted with 1-[2-(4-fluorophenyl)ethyl]piperazine of salts thereof to give the product.

REFERENCES:
T. Owa et al.: “Discovery of Novel Antitumor Sulfonamides Targeting G1 Phase of the Cell Cycle” J. Med. Chem., vol. 42, No. 19, 1999, pp. 3789-3799, XP002193774.
S. Swaminathan et al.: “N-Mannich Bases of 3-Substituted Indoles and Alkylation with Some N-Indolylmethyltrimethylammonium Iodides” J. Org. Chem., vol. 23, 1958, pp. 707-711, XP001063047.
F. Santanelo et al.: “A convenient synthesis of 9-hydroxy-3, 4,5, 6-tetrahydro-1H-azepino ' 5, 4, 3-cd! indole form 7-methoxyindole” Synth. Commun. , vol. 23, No. 19, 1993, pp. 2717-2726, XP001063048.
D. Sowmithran, K.J. Rajendra Prasad: “Heterocycles: Part 5—Synethesis of Carbazolyl-1-oxypropanolamine” Indian J. Chem. Sect. B, vol. 26, No. 1-12, 1987, pp. 277-278 XP001057373.

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