Starks Associates Inc.

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

Fred W Starks

Robert J Schultz

Jack L Parsons

Henryk Dubicki

N-(Phosphonoacetyl)-L-aspartic acid (PALA) compounds, especially novel PALA compounds, and methods for their preparation in large amounts are disclosed. These methods include preparation of certain PALA compounds such as PALA dibenzyl ester, disodium PALA, and the cyclohexylamine salt of dibenzyl PALA.

N-(phosphonacetyl)-L-aspartic acid salts with piperazine,

N-(Phosphonoacetyl)-L-aspartic acid compounds

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,

N-(Phosphonoacetyl)-L-aspartic acid compounds and methods for their

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. Particular aspects of these methods include: (1) initial preparation of the PALA moiety as the dibenzyl ester; (2) the complete removal of impurities in the form of acetic acid and sodium acetate from disodium PALA by turbulent flow precipitation; and (3) preparation and purification of the cyclohexylammonium salt of dibenzyl PALA which ultimately results in a purer final product.

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

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Kenmore, NY, United States of America

Fred W Starks