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The United States of America As Represented by the Department of Health

The United States of America As Represented by the Secretary of Health

Henryk Dubicki

Jack L Parsons

Fred W Starks

Suresh Marathe

Dan Vizine

Mark Sumner

An improved multi-step process for the production of 2-.beta.-D-ribofuranosylthiazole-4-carboxamide.

Process for the production of

A multi-step method of producing the compound methanesulfon-m-anisidide, 4'-(9-acridinylamino)-, acetate (VII), which may be in free base form and designated NSC 249992, also known as AMSA. This compound is produced by an elegant process from a starting material, 4-butyrylamino-3-methoxy-nitrobenzene, which is later transformed to methanesulfon-m-anisidide, 4'-amino- (IV) and is coupled or joined to 9-chloro-acridine, producing the chloride salt which is later converted to the acetate.

Multi-step process for the production of methanesulfon-m-anisidide,

Improved methods for preparation of the tetrasodium and disodium salts of N-(phosphonoacetyl)-L-aspartic acid (PALA) are disclosed. The present methods are well suited for preparation of these products in large amounts. A particular aspect of these methods includes a water-ethanol washing procedure for reducing impurities, including acetic acid, sodium acetate and ethanol, to an acceptable level.

Preparation of N-(phosphonoacetyl)-L-aspartic acid

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Lancaster, NY, United States of America

Henryk Dubicki