cas 88768-40-5, Cilazapril | Articles data ｜lookchem

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88768-40-5

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PROCESS FOR THE PREPARATION OF AN INTERMEDIATE OF CILAZAPRIL
The present invention relates to a process for the preparation of optically pure (S,S)-6-t-butoxycarbonyl-hexahydro-1-pyridazinylcarbonyl-1,3-dioxo-2-isoindolebutyric acid, an intermediate for the preparation of cilazapril.
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(2012/05/04)

A NOVEL PROCESS FOR THE PREPARATION OF CILAZAPRIL
Cilazapril is prepared in good yield using ethyl R-2-(nitro or halo substituted benzene sulfonyloxy)-4-phenyl butyrate. Thus, (1S,9S)-t-butyl octahydro-10-oxo-9-amino-6H-pyridazino[1,2-a][1,2]diazepine-1-carboxylate is reacted with ethyl R-2-(4-nitro benz
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Page 4-5

(2008/06/13)

ENANTIOMERICALLY PURE CILAZAPRIL,PROCESS FOR PREPARATION
The invention relates to enantiomerically pure cilazapril and a process for preparing enantiomerically pure cilazapril. The invention also relates to pharmaceutical compositions that include the enantiomerically pure cilazapril and use of said composition
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Page 5-6

(2008/06/13)

The Design and Synthesis of the Angiotensin Converting Enzyme Inhibitor Cilazapril and Related Bicyclic Compounds
The postulated binding functions for the active site of Angiotensin Converting Enzyme (A.C.E.), derived in an earlier study, have made possible the design of improved inhibitors.Consequently, (1S,9S)-9-octahydro-10-oxo-6H-pyridazodiazepine-1-carboxylic acid (Cilazapril), and related compounds, have been synthesized.They are very active inhibitors of A.C.E. and are highly potent antihypertensives in vivo.
Attwood, Michael R.,Hassall, Cedric H.,Kroehn, Antonin,Lawton, Geoffrey,Redshaw, Sally
p. 1011 - 1020
(2007/10/02)

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Chemical Properties

Appearance/Colour :Off-White Solid
Melting Point: 95-97 °C
Boiling Point: 598.1 °C at 760 mmHg
Flash Point:315.5 °C
Density: 1.26 g/cm³
Solubility:Chloroform (Slightly), Ethanol (Slightly, Sonicated), Methanol (Slightly)
Storage Temp.:2-8°C
Vapor Pressure: 3.73E-15mmHg at 25°C
Refractive Index: 1.591
PSA: 99.18000
LogP: 1.86220

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