1464851-21-5Relevant articles and documents
Preparation method of tenofovir intermediate
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Paragraph 0021-0038, (2017/08/28)
The invention discloses a preparation method of a tenofovir intermediate. The preparation method comprises the following steps: 1, contacting and reacting adenine with (Z)-1-halopropylene in an organic solvent in the presence of hexamethylphosphoramide to obtain (Z)-9-propenyladenine; and 2, reacting the (Z)-9-propenyladenine with metachloroperbenzoic acid under the catalysis of a chiral catalyst to obtain the tenofovir intermediate (R)-9-(2-hydroxypropyl)adenine, wherein the chiral catalyst is D-(-)-tartaric acid. The raw materials of the preparation method of the tenofovir intermediate are easy to obtain, so cost control is facilitated; the target product is obtained through introducing relative configuration Z shape alkene and carrying out selective oxidation without using a large amount of a chiral compound, so the product selectivity is good, and the yield is high; and the method has the advantages of no special strict conditions, mild reaction conditions, and convenience in amplified production operation and industrial application promotion.
Synthesis of (E)-9-(Propen-1-yl)-9 H-adenine, a mutagenic impurity in tenofovir disoproxil fumarate
Chavakula, Ramadas,Mutyala, Narayanarao,Chennupati, Srinivasarao
, p. 336 - 340 (2013/07/25)
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