AMINOEPOXIDE PREPARATION ACCOMPLISHED AS CONTINUOUS IN SITU SYNTHESIS Russian patent published in 2002 - IPC

Abstract RU 2194045 C2

FIELD: organic synthesis. SUBSTANCE: invention relates to preparing aminoepoxides, in particular, chiral ones, that can be applied in chemical and pharmaceutical industries. According to invention, protected aminoaldehyde reacts with halomethyl-organometallic reagent in suitable solvent at temperature above minus 80 C. More particularly, halomethyl-organometallic reagent forms in the course of reaction of organometallic reagent with dihalomethane. Process includes following steps: feeding protected aminoaldehyde into the first mixing zone and simultaneously feeding dihalomethane into the same zone to come into contact with protected aminoaldehyde and to give the first mixture; feeding indicated organometallic reagent into the second mixing zone operated at temperature below 0 C and simultaneously feeding the first mixture into the same zone to provide contact of the first-mixture dihalomethane with organometallic reagent to form reaction mixture containing desired halomethyl-organometallic reagent; feeding thus formed reaction mixture into the third mixing zone therefrom reaction products of protected aminoaldehyde and halomethyl-organometallic reagent are discharged. Resulting aminoepoxides are useful as intermediates in synthesis of pharmaceutical preparations, for example HIV protease inhibitors. EFFECT: enhanced process efficiency. 13 cl, 34 ex

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RU 2 194 045 C2

Authors

Liu Chin

Ng Dzhon S.

Bekhling Dzhejms R.

Kempbell Artur L.

Dates

2002-12-10Published

1997-12-19Filed