Eli Lilly and Company

Thomas J Kress

James P Wepsiec

Michael J Martinelli

M Robert Leanna

Barry C Peterson

Kevin L Haehl

James E Audia

Vincent Patrick Rocco

David Lee Varie

Blake L Neubauer

Loretta A McQuaid

Larry L Moore

Edward F Szymanski

Separation of 5-nitroquinoline and 8-nitroquinoline

A series of benzoquinolin-3-ones are pharmaceuticals effective in treating conditions consequent on both Type I and Type II 5.alpha.-reductase.

5.alpha.-reductase inhibitors

A series of benzoquinolin-3-ones are pharmaceuticals effective in treating conditions consequent on both Type I and Type II 5.alpha.-reductase and their preparation is disclosed.

Process for preparation of benzo[f]quinolinones

New intermediates, and processes therefor, provide an efficient method for deriving 4-amino-1,2,2a,3,4,5-hexahydrobenz[cd]indoles, which are themselves intermediates to useful CNS agents, from the Kornfeld-Woodward ketone and like compounds. Preferred embodiments provide means for the preparation of substantially pure enantiomers of the desired 4-amino-1,2,2a,3,4,5-hexahydrobenz[cd]indole.

Intermediates to 4-amino- hexahydrobenz (cd) indoles and processes

Crystalline 4-(di-n-propyl)amino-6-aminocarbonyl-1,3,4,5-tetrahydrobenz[cd]indole hippurate and its method of preparation and use are provided.

Crystalline salt of

New intermediates, and processes therefor, provide an efficient method for deriving 4-amino-1,2,-2a,3,4,5-hexahydrobenz[cd]indoles, which are themselves intermediates to useful CNS agents, from the Kornfeld-Woodward ketone and like compounds. Preferred embodiments provide means for the preparation of substantially pure enantiomers of the desired 4-amino-1,2,2a,3,4,5-hexahydrobenz[cd]indole.

Intermediates to 4-amino-hexahydrobenz[cd]indoles and processes therefor

4-Amino-6-iodo-1,2,2a,3,4,5-hexahydrobenz[ cd]indoles are useful intermediates to 4-amino-1,3,4,5-tetrahydrobenz [cd]indoles containing aminocarbonyl or alkoxycarbonyl substituents in the 6-position which are useful for the treatment of various disorders of the central nervous system.

4-amino-6-iodo-hexahydrobenz(cd)indoles

The reaction of formamide at high temperature with a 4-halo-5-hydroxy-2(5H)-furanone provides high yields of 5-chloro or 5-bromopyrimidines.

Process for preparing 5-halopyrimidines

2-Amino-5-chloropyridine is prepared by chlorinating 2-aminopyridine in a strongly acidic medium. 2-Amino-5-chloropyridine is a useful intermediate in the preparation of chloro-substituted-imidazo-pyridine herbicides.

Process for preparing 2-amino-5-chloropyridine

The process for brominating pyrimidine which comprises reacting bromine at an elevated temperature with the hydrogen halide addition salt of pyrimidine in an organic solvent substantially inert to the action of bromine under the conditions of the process. The process is also shown to be applicable to other nitrogen-containing heterocycles.

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Indianapolis, IN, United States of America

Thomas J Kress