RU2010121534A - METHOD FOR PRODUCING 5'-AMINOCARBONYLPHOSPHONATES OF NUCLEOSIDES AND METHOD FOR PRODUCING Trimethylsilyl Chloride Hydride of Ethoxycarbonylphosphonic Acid - Google Patents

METHOD FOR PRODUCING 5'-AMINOCARBONYLPHOSPHONATES OF NUCLEOSIDES AND METHOD FOR PRODUCING Trimethylsilyl Chloride Hydride of Ethoxycarbonylphosphonic Acid Download PDF

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Publication number
RU2010121534A
RU2010121534A RU2010121534/04A RU2010121534A RU2010121534A RU 2010121534 A RU2010121534 A RU 2010121534A RU 2010121534/04 A RU2010121534/04 A RU 2010121534/04A RU 2010121534 A RU2010121534 A RU 2010121534A RU 2010121534 A RU2010121534 A RU 2010121534A
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RU
Russia
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producing
acid
ethoxycarbonylphosphonic
aminocarbonylphosphonates
nucleosides
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RU2010121534/04A
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Russian (ru)
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RU2446169C2 (en
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Максим Владимирович Ясько (RU)
Максим Владимирович Ясько
Наталья Александровна Голубева (RU)
Наталья Александровна Голубева
Александр Валерьевич Шипицын (RU)
Александр Валерьевич Шипицын
Анастасия Львовна Хандажинская (RU)
Анастасия Львовна Хандажинская
Роберт Шалвович Бибилашвили (RU)
Роберт Шалвович Бибилашвили
Александр Васильевич Кононов (RU)
Александр Васильевич Кононов
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Закрытое акционерное общество "Производственно-коммерческая Ассоциация АЗТ" (RU)
Закрытое акционерное общество "Производственно-коммерческая Ассоциация АЗТ"
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Priority to RU2010121534/04A priority Critical patent/RU2446169C2/en
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Abstract

1. Способ получения 5'-аминокарбонилфосфонатов нуклеозидов, включающий взаимодействие фосфонилирующего реагента с нуклеозидом в инертном апротонном растворителе и обработку промежуточных 5'-этоксикарбонилфосфонатов водным раствором аммиака, отличающийся тем, что с целью упрощения технологического процесса в качестве фосфонилирующего реагента используют хлорангидрид триметилсилильного эфира этоксикарбонилфосфоновой кислоты, а фосфорилирование проводят в присутствии диметилформамида. ! 2. Способ получения хлорангидрида триметилсилильного эфира этоксикарбонилфосфоновой кислоты, заключающийся в последовательной обработке триэтилфосфоноформиата сначала триметилбромсиланом, а затем пентахлоридом фосфора или тионилхлоридом. 1. A method of producing 5'-aminocarbonylphosphonates of nucleosides, comprising reacting a phosphonylating reagent with a nucleoside in an inert aprotic solvent and treating the intermediate 5'-ethoxycarbonylphosphonates with an aqueous solution of ammonia, characterized in that trimethylsulfonyl ether trimethylsulfonyl ether trimethylsulfonate acid is used as a phosphonylating reagent. and phosphorylation is carried out in the presence of dimethylformamide. ! 2. A method of producing ethoxycarbonylphosphonic acid trimethylsilyl ester chloride, which consists in sequentially treating triethyl phosphonoformate first with trimethyl bromosilane and then with phosphorus pentachloride or thionyl chloride.

Claims (2)

1. Способ получения 5'-аминокарбонилфосфонатов нуклеозидов, включающий взаимодействие фосфонилирующего реагента с нуклеозидом в инертном апротонном растворителе и обработку промежуточных 5'-этоксикарбонилфосфонатов водным раствором аммиака, отличающийся тем, что с целью упрощения технологического процесса в качестве фосфонилирующего реагента используют хлорангидрид триметилсилильного эфира этоксикарбонилфосфоновой кислоты, а фосфорилирование проводят в присутствии диметилформамида.1. A method of producing 5'-aminocarbonylphosphonates of nucleosides, comprising reacting a phosphonylating reagent with a nucleoside in an inert aprotic solvent and treating the intermediate 5'-ethoxycarbonylphosphonates with an aqueous solution of ammonia, characterized in that trimethylsulfonyl ether trimethylsulfonyl ether trimethylsulfonate acid is used as a phosphonylating reagent. and phosphorylation is carried out in the presence of dimethylformamide. 2. Способ получения хлорангидрида триметилсилильного эфира этоксикарбонилфосфоновой кислоты, заключающийся в последовательной обработке триэтилфосфоноформиата сначала триметилбромсиланом, а затем пентахлоридом фосфора или тионилхлоридом. 2. A method of producing ethoxycarbonylphosphonic acid trimethylsilyl ester chloride, which consists in sequentially treating triethyl phosphonoformate first with trimethyl bromosilane and then with phosphorus pentachloride or thionyl chloride.
RU2010121534/04A 2010-05-28 2010-05-28 Method of producing 5'-aminocarbonylphosphonates of nucleosides and method of producing acyl chloride of trimethylsilyl ether of ethoxycarbonylphosphonic acid RU2446169C2 (en)

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RU2010121534/04A RU2446169C2 (en) 2010-05-28 2010-05-28 Method of producing 5'-aminocarbonylphosphonates of nucleosides and method of producing acyl chloride of trimethylsilyl ether of ethoxycarbonylphosphonic acid

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RU2010121534/04A RU2446169C2 (en) 2010-05-28 2010-05-28 Method of producing 5'-aminocarbonylphosphonates of nucleosides and method of producing acyl chloride of trimethylsilyl ether of ethoxycarbonylphosphonic acid

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RU2010121534A true RU2010121534A (en) 2011-12-10
RU2446169C2 RU2446169C2 (en) 2012-03-27

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN113473994A (en) * 2018-12-27 2021-10-01 长效药物有限责任公司 Combination of antiviral agents, kits and methods of treatment based thereon

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5132414A (en) * 1990-05-10 1992-07-21 Dana-Farber Cancer Institute, Inc. Dideoxynucleoside-5'-phosphonoformic acid compounds

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN113473994A (en) * 2018-12-27 2021-10-01 长效药物有限责任公司 Combination of antiviral agents, kits and methods of treatment based thereon

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Effective date: 20180426