Method for the preparation of 5-cyanophthalide

Details Method for the preparation of 5-cyanophthalide Method for the preparation of 5-cyanophthalide

2005-06-28

2005-06-28

Stockton, Laura L. (Department: 1626)

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

C549S467000

Reexamination Certificate

active

06911548

ABSTRACT:
A method for the preparation of 5-cyanophthalide comprising treatment of a compound of formula IVwherein X is O or S;R1-R2are each independently selected from hydrogen and C1-6alkyl, or R1and R2together form a C2-5alkylene chain thereby forming a spiro-ring; R3is selected from hydrogen and C1-6alkyl, R4is selected from hydrogen, C1-6alkyl, a carboxy group or a precursor group therefore, or R3and R4together form a C2-5alkylene chain thereby forming a spiro-ring; with a dehydration agent or alternatively where X is S, thermally cleavage of the thiazoline ring or treatment with a radical initiator, such as peroxide or with light, to form 5-cyanophthalide, which is an important intermediate used in the preparation of the antidepressant drug citalopram.

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