Bristol-Myers Company

Bristol-Myers Squibb Compnay

Henry G Howell

John E Starrett, Jr

John C Martin

Muzammil M Mansuri

Carl E Fuller

Chester Sapino, Jr

Steven P Brundidge

Richard A Partyka

Alexander T Shulgin

Robert T Standridge

Chon-Hong Tann

Chou Hong-Tann

There are disclosed novel processes for producing 2',3'-dideoxy-2'3'-didehydronucleosides, for example, 2',3'-dideoxy-2',3'-didehydrothymidine in high yields and on a large scale. The compounds so-produced are useful as antiviral agents, especially as agents effective against the human immunodeficiency viruses (HIV).

Production of 2',3'-dideoxy-2',3'-didehydronucleosides

Process for producing 1-halo-2-deoxy-2-fluoroarabinofuranoside derivatives bearing protective ester groups from 1,3,5-tri-O-acylribofuranose; the 1-halo compounds are intermediates in the synthesis of therapeutically active nucleosidic compounds.

Nucleoside process

An improved and novel process is provided for the reduction of isocyanate groups in organic compounds to formamide groups by catalytic hydrogenation with a noble metal catalyst. The process allows preparation of formamides in consistently high yields from all types of isocyanates.

Hydrogenation process

Compounds of the formula ##STR1## wherein R.sup.1 is Cl, Br, (lower)alkylthio or ##STR2## in which R.sup.3 is H or (lower)alkyl including the racemic mixtures and the dextrorotatory and levorotatory isomers, and the pharmaceutically acceptable non-toxic salts thereof have been found to enhance the learning capacity of mammals, including man, and to improve the mental alertness and attitudes of geriatrics without producing the undesirable stimulant side effects associated with the use of amphetamines.

2-Amino-1-(2,5-dimethoxyphenyl)-butanes

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East Syracuse, NY, United States of America

Henry G Howell