Keystone Biomedical, Inc.

Cyclo.sub.3 Pss Medical Systems, Inc.

Larry A Gaudioso

Christopher G Anderson

Michael A Weglarz

Frank P McNeil

A process for the synthesis of an Exochelin comprising the steps of generating L-N-[(2-benzyloxy-(benzoyl)] serine or L-N-[2-benzyloxy (benzoyl)] threonine, creating L-N-t-Boc-.epsilon.-hydroxynorleucine and reacting same to produce L-N-Boc-.epsilon.-bromonorleucine trimethylsilylethyl ester, providing a dicarboxylic acid and forming an O-benzyl methyl hydroxamate from the dicarboxylic acid, coupling the O-benzyl methyl hydroxamate with the L-N-Boc-.epsilon.-bromonorleucine trimethylsilylethyl ester to give an L-N.sup.2 -Boc-N.sup.6 -methyl,N.sup.6 -(benzyloxy) lysine 2-trimethylsilylethyl ester which incorporates the dicarboxylic acid as modified above, removing the N-tert-butoxycarbonyl protecting group from the L-N.sup.2 -Boc-N.sup.6 -methyl, N.sup.6 -(benzyloxy) lysine 2-trimethylsilylethyl ester to yield a substituted lysine, and coupling the same with the L-N-[2-benzyloxy (benzoyl) serine or -threonine to yield a 2-trimethyl silylethyl ester of dibenzyl Exochelic acid, transforming the 2-trimethyl silylethyl ester of dibenzyl Exochelic acid to dibenzyl Exochelic acid, preparing benzyl epi-cobactin, forming an ester bond between the dibenzyl Exochelic acid and benzyl epi-cobactin to form an intermediate, and, hydrogenolytically removing three benzyl groups from said intermediate, resulting in the synthesized Exochelin. More particularly, a synthesis for Exochelin 786SM (R) is disclosed wherein the dicarboxylic acid is suberic acid and the serine form is utilized.

Process for the synthesis of exochelins

A method and a composition for disinfecting matter or materials such as medical instruments, operating rooms, examining tables, walls, windows, floors, solutions, porous substances and the like contaminated with bacteria, bacterial spores, fungi, or viruses is disclosed. The composition consists of a mixture of a peroxymonosulfate and a carbonyl-containing compound and reaction products thereof and is preferably dioxirane formed by in situ oxidation of a ketone or aldehyde by the peroxymonosulfate in aqueous solution. Carbonyl-containing compounds that have been tested include acetone, 2-pentanone, 4-hydroxy-4-methyl-2-pentanone, and camphorsulfonic acid. The method includes providing a solution containing the dioxirane reaction mixture and contacting the matter or materials with it at room temperature for a time sufficient to disinfect and sterilize the matter or materials.

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Salt Lake City, UT, United States of America

Larry A Gaudioso