Preparation of asymmetric cyclic ureas through a monoacylated diamine intermediate

The present invention concerns an improved process for the preparation of asymmetric cyclic ureas as well as intermediates in the preparation of asymmetric cyclic ureas. In the process, a diamine of formula (I-a) is selectively monoacylated to give an asymmetric monoacylated diamine which can be con...

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Main Authors HARRIS, GREGORY D, ANZALONE, LUIGI, STONE, BENJAMIN R. P, VALVIS, IOANNIS I., FORTUNAK, JOSEPH M
Format Patent
LanguageEnglish
Published 11.10.2002
Edition7
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
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Abstract The present invention concerns an improved process for the preparation of asymmetric cyclic ureas as well as intermediates in the preparation of asymmetric cyclic ureas. In the process, a diamine of formula (I-a) is selectively monoacylated to give an asymmetric monoacylated diamine which can be converted into asymmetric intermediates. The asymmetric intermediates can be further alkylated, cyclized, and/or modified to give compounds which are useful as HIV protease inhibitors for the treatment of HIV infection. The invention allows for scalable preparation of a wide variety of asymmetrical cyclic ureas.
AbstractList The present invention concerns an improved process for the preparation of asymmetric cyclic ureas as well as intermediates in the preparation of asymmetric cyclic ureas. In the process, a diamine of formula (I-a) is selectively monoacylated to give an asymmetric monoacylated diamine which can be converted into asymmetric intermediates. The asymmetric intermediates can be further alkylated, cyclized, and/or modified to give compounds which are useful as HIV protease inhibitors for the treatment of HIV infection. The invention allows for scalable preparation of a wide variety of asymmetrical cyclic ureas.
Author ANZALONE, LUIGI
HARRIS, GREGORY D
VALVIS, IOANNIS I.
FORTUNAK, JOSEPH M
STONE, BENJAMIN R. P
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– fullname: FORTUNAK, JOSEPH M
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Snippet The present invention concerns an improved process for the preparation of asymmetric cyclic ureas as well as intermediates in the preparation of asymmetric...
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SubjectTerms CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
Title Preparation of asymmetric cyclic ureas through a monoacylated diamine intermediate
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