Hoffmann-La Roche Inc.

Pasquale N Confalone

Milan R Uskokovic

Giacomo Pizzolato

Elizabeth D Lollar

Enrico G Baggiolini

Marianne Rouge

Thiophene derivatives having utility as blood lipid lowering agents and as antiobesity agents are disclosed.

Novel thiophene derivatives

Novel thiophene compounds having utility as biotin intermediates and blood lipid lowering agents, as well as related processes and intermediates, are disclosed.

Novel thiophene compounds

A novel process for the preparation of biotin is disclosed wherein said process employs inexpensive starting materials and reagents resulting in the obtention of biotin devoid of the biologically inactive stereoisomers.

Novel cycloheptathiophene intermediates for the synthesis of biotin

The invention relates to synthetic processes to produce the known pharmacologically active 8-methoxypsoralen and derivatives thereof. Also disclosed are various novel intermediates utilized in these processes.

Coumarin derivatives to produce 8-methoxypsoralen

Cycloheptathiophene derivatives

8-Methoxypsoralen derivatives

Synthesis of biotin

Synthesis of biotin from 4-carbomethoxy-2-(4,5-dihydrothiophen-3(2H)-one)-valeric acid methyl ester, and thiophene intermediates in this synthesis.

A novel procedure for the preparation of biotin, using cysteine as the starting material is disclosed. This process results in the obtention of pure d-biotin thus obviating the need for a chemical resolution. Novel intermediates are also disclosed.

2,3,3A,6,7,7A-Hexahydro-thieno[3,2-b]pyridin-(4H)5-ones

Synthesis of biotin from 4-carbomethoxy-2-(4,5-dihydrothiophen-3(2H)-one)-valeric acid methyl ester, and dihydrothiophene intermediates in this synthesis.

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Bloomfield, NJ, United States of America

Pasquale N Confalone