PROCESS FOR THE PREPARATION OF AMINO ALCOHOL DERIVATIVES OR SALTS THEREOF
The present invention relates to a process for the preparation of amino alcohol derivatives or salts thereof. In particular the present invention relates to process for the preparation of amino alcohol derivatives or salts thereof which may be used as intermediates in the preparation of HIV reverse transcriptase inhibitors, more preferably Carbovir and Abacavir. The present invention more specifically relates to a process for the preparation of (1S,4R)-4-amino-2-cyclopentene-1-methanol of Formula IIIa. The present invention also specifically relates to process for the preparation of Abacavir sulfate of Formula II using compound of Formula IIIa prepared according to the process of the present invention.
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Paragraph 0061; 0062; 0063; 0064; 0065
(2017/09/02)
Process for the Preparation of Abacavir
Process for removal of the amino protective group of a N-acylated [(1S,4R)-4-[2-amino-6-(cyclopropylamino)-9H-purin-9-yl]-cyclopent-2-enyl]methanol of formula (II) where R═H or a (C1-C4)-alkyl, using an inorganic base in a mixture of water and alcohol, to yield abacavir or its salts. The process proceeds very fast and the product can be obtained in high yield and purity.
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Page/Page column 2-3
(2010/02/16)
Process for the preparation of abacavir
Process for removal of the amino protective group of a N-acylated {(1S,4R)-4-[2-amino-6-(cyclopropylamino)-9H-purin-9-yl]-cyclopent-2-enyl}methanol of formula (II) where R = H or a (C1-C4)-alkyl, using an inorganic base in a mixture of water and alcohol, to yield abacavir or its salts. The process proceeds very fast and the product can be obtained in high yield and purity.
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Page/Page column 4
(2008/06/13)
Process for the preparation of abacavir
Process for the preparation of abacavir starting from compound of formula (IV) where R1 is a (C1-C4)-alkyl radical comprising first reacting said compound (IV) with anhydrous hydrochloric acid/(C1-C6)-alcohol, and then with tri(C1-C4)-alkyl orthoformate, in the absence of water, followed by reacting the compound obtained with cyclopropylamine and hydrolysing the compound obtained to yield abacavir or its salts.
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Page/Page column 7
(2008/12/06)
NOVEL CRYSTALLINE FORMS OF ABACAVIR SULFATE
The present invention relates to novel crystalline forms of abacavir sulfate, to processes for their preparation and to pharmaceutical compositions containing them.
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Page 3
(2008/06/13)
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