CAS: 180587-75-1; 9-[(2S)-2-(Diethoxyphosphorylmethoxy)Propyl]Purin-6-Amine

上下游产品

diethyl (p-toluenesulfonyloxymethane)phosphonate (R)-9-(2-hydroxypropyl)adenine diethyl (1-hydroxymethyl)phosphonate adenine tenofovir tenofovir disoproxil

📜腺嘌呤置于甲基氯化镁,Potassium Hydroxide,叔丁醇体系中,用 四氢呋喃,环己烷,N,N-二甲基甲酰胺 用作溶剂,化学反应 3.0H,反应生成替诺福韦二乙酯
参考文献:替诺福韦酯富马酸酯的改进工艺
标题:替诺福韦酯富马酸酯的改进工艺
摘要:评估并优化了目前用于制备替诺福韦富马酸替诺福韦(1)的三步生产路线,从而提高了产量,简化了流程并实现了绿色环保.工艺路线的关键改进包括通过用1:1格氏试剂和叔丁醇代替有问题的叔丁醇镁(mtb)来改进第二阶段.实现了一种几乎无溶剂的方法的开发,并建立了可以分离出纯二乙基膦酸酯(8)的后处理和纯化方案.
Doi:10.1021/acs.Oprd.5B00364

专利信息

专利号:US-10155007-B2
优先权日:2014-10-29
标 题:Synthesis method for improved tenofovir disoproxil fumarate using ion-exchange resin and method for preparing oral dissolving film form using the same
发明人：KIM DONG-JIN; KOO CHANG-HUI; CHO IL-HEE; LEE SUNG-BAE; HAN DONG-HOON
权利人:FIRSON
摘要:The present invention relates to a synthesis method of preventing the formation of impurities and byproducts in the synthesis of tenofovir disoproxil fumarate (Teno-DF) used as a medicine for hepatitis B and HIV treatment due to its function to promote bioactivities. In the synthesis method of the present invention, an ion-exchange resin (Dowex 50W hydrogen form, sulfonic acidic cation exchange resin) is used to enhance the yield and purity of the compound. The present invention also relates to a method of preparing an oral dissolving film dosage form in the manufacture of a medicine using the tenofovir compound with high purity obtained by the synthesis method of the present invention as an effective ingredient.

专利号:EP-0998480-B1
优先权日:1997-07-25
标 题:Nucleotide analog composition and synthesis method
发明人：MUNGER JOHN D JR; ROHLOFF JOHN C; SCHULTZE LISA M
权利人:GILEAD SCIENCES INC
摘要:The invention provides a composition comprising bis(POC)PMPA and fumaric acid (1:1). The composition is useful as an intermediate for the preparation of antiviral compounds, or is useful for administration to patients for antiviral therapy or prophylaxis. The composition is particularly useful when administered orally. The invention also provides methods to make PMPA and intermediates in PMPA synthesis. Embodiments include lithium t-butoxide, 9-(2-hydroxypropyl) adenine and diethyl p-toluenesulfonylmethoxy-phosphonate in an organic solvent such as DMF. The reaction results in diethyl PMPA preparations containing an improved by-product profile compared to diethyl PMPA made by prior methods.

专利号:US-8507463-B2
优先权日:2005-06-13
标题 :Nucleotide analogue prodrug and the preparation thereof
发明人：YUAN JIANDONG
权利人:YUAN JIANDONG; JIANGSU CHIA TAI TIANQING PHAR; BRIGHTGENE BIO MEDICAL TECHNOLOGY CO LTD
摘要:The present invention provides: 1) Derivative solid form of 9-[2-(R)-[bis[pivaloyloxymethoxy]-phosphinylmethoxy]propyl]adenine (bis-POM PMPA, abbreviated as TD hereinafter), including crystalline form A and form B of TD, TD fumarate salts and cyclodextrin inclusion complex of TD; 2) Synthesis and purification methods of TD and Solidification method of TD oil, including converting TD oil to crystalline TD in Form A and Form B, solid TD salts and cyclodextrin inclusion complex of TD; 3) Stable pharmaceutical compositions containing TD derivatives and their preparation; 4) The use of the above TD derivatives in the antiviral treatments, especially in the treatment of HIV, HBV, CMV, HSV-1, HSV-2 and human Herpes virus infections.

专利号:KR-20160052905-A
优先权日:2014-10-29
标 题:Ion exchanging process method for Tenofovir disoproxil fumarate in manufacturing synthesis and a preparation method of the Fast Dissolving Films for Oral Dosage of Tenofovir disoproxil fumarate

专利号:KR-20060038451-A
优先权日:1997-07-25
标 题 :An intermediate for the preparation of pmpa and synthesis method

专利号:JP-2002511098-A
优先权日:1997-07-25
标 题 :Nucleotide analog compositions and methods of synthesis