1256490-31-9Relevant articles and documents
Enzyme-Catalyzed Kinetic Resolution of Chiral Precursors to Antiviral Prodrugs
Xiang, Dao Feng,Bigley, Andrew N.,Desormeaux, Emily,Narindoshvili, Tamari,Raushel, Frank M.
, p. 3204 - 3211 (2019)
Nucleoside analogues are among the most common medications given for the treatment of viral infections and cancers. The therapeutic effectiveness of nucleoside analogues can be dramatically improved by phosphorylation. The ProTide approach was developed u
(S)- 2 - [(s)- (4 - nitro - phenoxy) - phenoxy - phosphoryl amino] isopropyl propionate preparation method
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Paragraph 0023; 0029; 0030; 0031, (2017/08/25)
The invention relates to a preparation method of (s)-2-[(s)-(4-nitro-phenoxy)-phenoxy-phosphoryl amino] isopropyl propionate. The (s)-2-[(s)-(4-nitro-phenoxy)-phenoxy-phosphoryl amino] isopropyl propionate, which is excellent in chemical purity and optical purity, is prepared by the following steps: preparing a compound as shown in a formula (III) from phenoxy dichlorophosphite as shown in a formula (I) and nitrophenol as shown in a formula (II), preparing a compound as shown in formula (V) from the compound as shown in the formula (III) and L-alanine isopropyl ester hydrochloride, and implementing solvent recrystallization on the compound as shown in the formula (V). The preparation method disclosed by the invention has the beneficial effects that the method for preparing the (s)-2-[(s)-(4-nitro-phenoxy)-phenoxy-phosphoryl amino] isopropyl propionate is simple in technological process and convenient to operate, and meanwhile the method is high in both purity and yield and is applicable to mass production.
DIOXOLANE ANALOGUES OF URIDINE FOR THE TREATMENT OF CANCER
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Page/Page column 52; 53, (2016/03/22)
The invention provides compounds of formula (I), wherein: R1 is OR11, or NR5R5'; R2 is H or F; R5 is H, C1-C6alkyl, OH, C(=O)R6, O(C=O)R6 or O(C=O)OR6; R5′ is H or C1-C6alkyl; R6 is C1-C6alkyl or C3-C7cycloalkyl; R13 is H, phenyl, pyridyl, benzyl, indolyl or naphthyl wherein the phenyl, pyridyl, benzyl, indolyl and naphthyl is optionally substituted with 1, 2 or 3 R22; and the other variables are as defined in the claims, which are of use in the treatment of cancer, and related aspects.