Method of preparation of...

Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...

Reexamination Certificate

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Reexamination Certificate

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06894167

ABSTRACT:
A new method is described here for the synthesis of (S)-N-tert-butyl-1,2,3,4-tetrahydroiso-quinoline-3-carboxamide comprising the following steps:a) (3S)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid is reacted with formic acid to give the compound of formula:b) the compound thus obtained is reacted with tert-butylamine to give the compound of formula:c) the compound thus obtained is then treated with acids to give the desired compound.The method in question makes it possible to obtain (S)-N-tert-butyl-1,2,3,4-tetrahydroiso-quinoline-3-carboxamide with high yields and purity without using toxic and hazardous reagents.

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XP-000889687, Gohring, Wolfgang, et al., “Synthesis of the HIV-Proteinase Inhibitor Saquinavir: A Challenge for Process Research”, Chimia, AARAU, CH, vol. 50, No. 11, 1996, pp. 532-537.

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