Abstract:
1,6-Dihydro-4-phenyl-2,5,3-benzodioxazocine (1), 1,4-dihydro-3H2,3-benzoxazine-3-carboxamide (1''a), N-alkyl-1,4-dihydro-3H-2,3benzoxazine-3-carboxamides (1''b), 1,4-dihydro-3H-2,3-benzoxazine3-carboxamidine (1''c) and its acid addition salts, process for the preparation thereof and novel intermediates prepared by said processes. Compounds 1, 1''a, and 1''b principally exhibit antilipemic activity. Compound 1''c is useful for preparing mothproofing agents and inhibitors that can be used in the acid pickling of steel.
Abstract:
1,4-DIHYDRO-3H-2,3-BENZOXAZINE IS REACTED WITH HALOPHENYL CHLOROFORMATE TO FORM HALOPHENYL ESTERS OF 1,4DIHYDRO-3H-2,3-BENZOXAZINE-3-CARBOXYLIC ACID. THE 1,4DIHYDRO-3H-2,3-BENZOXAZINE-3-CARBOXYLIC ACID HALOPHENYL ESTERS HAVE UTILITY AS ANTIFUNGAL AND ANTILIPEMIC AGENTS.
Abstract:
Antibiotic AT-125, producible by culturing Streptomyces sviceus in an aqueous nutrient medium has the following structure: The absolute configuration of AT-125 was determined to be L-( Alpha S,5S)- Alpha -amino-3-chloro-2-isoxazoline-5-acetic acid. It is an amphoteric compound and can exist in different ionic forms according to the pH of the environment. At low pH, AT-125 exists in the acid-addition salt form, at a higher pH in a zwitterion form, and at a still higher pH in a metal salt form. AT-125 inhibits the growth of Bacillus subtilis, Saccharomyces pastorianus, Penicillium oxalicum, Candida albicans, Saccharomyces cerevisiae and Escherichia coli, and can be used to inhibit such microorganisms in various environments.
WHEREIN R IS HYDROGEN OR T-(BUTYL, PHTHALIMIDOMETHYL AND PHENACYL. A-METHYLBIOTIN AND ITS ESTERS HAVE THE FOLLOWING FORMULA:
4-(R-OOC-C(-CH3)-(CH2)3-)HEXAHYDROTHIENO(3,4-D)-
IMIDAZOL-2-ONE
WHEREIN R IS AS DEFINED ABOVE. A-METHYLDETHIOBIOTIN, WHERE R IS HYDROGEN IN FORMULA I, AND A-METHYLBIOTIN, WHERE R IS HYDROGEN IN FORMULA II, ARE PRODUCED IN A LYDIMYCIN FERMENTATION. THESE COMPOUNDS ARE ACTIVE AGAINST MYCOBACTERIUM AVIUM AND CAN BE USED TO CONTROL THIS MICROORGNISM WHICH IS A KNOWN PRODUCER OF GENERALIZED TUBERCULOSIS IN BIRDS AND RABBITS.