专利号:US-2023287032-A1 优先权日:2020-08-14 标 题:Synthesis of fluorinated nucleotides 发明人:CHUNG CHEOL KEUN; LIU ZHIJIAN; MALIGRES PETER E; MAO EDNA; OBLIGACION JENNIFER V; PHILLIPS ERIC M; PIRNOT MICHAEL; POIRIER MARC; SONG ZHIGUO JAKE; WANG TAO 权利人:CHUNG CHEOL KEUN; LIU ZHIJIAN; MALIGRES PETER E; MAO EDNA; OBLIGACION JENNIFER V; PHILLIPS ERIC M; PIRNOT MICHAEL; POIRIER MARC; SONG ZHIGUO JAKE; WANG TAO; MERCK SHARP & DOHME LLC 摘要:The present invention relates to efficient processes useful in the preparation of fluorinated nucleosides, such as (O—{[(2R,3R,4S,5R)-5-(6-amino-9H-purin-9-yl)-4-fluoro-3-hydroxyoxolan-2-yl]methyl}O,O-dihydrogen phosphorothioate, also known as 2′-(S)-fluoro-thio-adenosine monophosphate or 2′-F-thio-AMP. Such fluorinated nucleosides may be useful as a biologically active compound and or as an intermediate for the synthesis of more complex biologically active compounds. The present invention also encompasses intermediates useful in the disclosed synthetic processes and the methods of their preparation.
专利号:US-2006058532-A1 优先权日:2004-09-10 标 题:Process for the scalable synthesis of 1,3,4,9-tetrahydropyrano[3,4-b]-indole derivatives 发明人:CHEW WARREN; CHEAL GLORIA K; LUNETTA JACQUELINE F; DEMERSON CHRISTOPHER A 权利人:CHEW WARREN; CHEAL GLORIA K; LUNETTA JACQUELINE F; DEMERSON CHRISTOPHER A 摘要:The invention is directed to a process of synthesizing compounds of formula (VI): n n nwherein R 1- R 9 , R 3′ , R 4′ and Y are as set forth in the specification, and said method is useful for large scale synthesis thereof. The invention is also directed to useful intermediates for synthesizing the compounds of formula (VI) and processes of preparing said intermediates.
专利号:US-2008280855-A1 优先权日:2005-06-22 标 题 :Process For the Production of Intermediates For the Preparation of Tricyclic Benzimidazoles 发明人:CHIESA MARIA VITTORIA; PALMER ANDREAS; BUHR WILM; ZIMMERMANN PETER JAN; BREHM CHRISTOF; SIMON WOLFGANG-ALEXANDER; POSTIUS STEFAN; KROMER WOLFGANG; ZANOTTI-GEROSA ANTONIO 权利人:NYCOMED GMBH 摘要:The invention relates to a process for the synthesis of compounds of the formula 1-a and compounds of the formula 1-b. n n n n n n n n n n The compounds of the formula 1-a and the compounds of the formula 1-b, in which the substituents R1, R2, R3, and Ar have the meanings indicated in the description, are valuable intermediates for the preparation of pharmaceutically active compounds.
专利号:US-2007208164-A1 优先权日:2006-02-27 标题:Methods of synthesizing radiolabeled 3-cyano[14C]quinolines 发明人:OLSZEWSKI JOHN D; MAY MICHAEL K; BERGER DAN M 权利人:WYETH CORP 摘要:The present invention is directed to radiolabeled 3-cyanoquinolines of the formula: n n nand methods of synthesizing the same, wherein G 1 , G 2 R 1 , R 4 , Z, X, and n are as defined herein. n nThe present invention is also directed to a radiolabeled intermediate compounds of formula (VII): n n nwherein PG, G 1 , R 1 , R 4 , R 10 , and R 11 are as defined herein, and synthesis of the same.
专利号:US-10077242-B2 优先权日:2014-12-01 标题 :Convergent approach to the total synthesis of telmisartan via a suzuki cross-coupling reaction 发明人:GUPTON FRANK; MARTIN ALEX; SIAMAKI ALI; BELECKI KATHERINE 权利人:UNIV VIRGINIA COMMONWEALTH 摘要:Methods of synthesizing the angiotensin II receptor antagonist telmisartan in high yield and purity are provided. The methods involve the coupling of two structurally distinct benzimidazole units via a Suzuki cross-coupling reaction. Methods of regioselectively synthesizing one of the benzimidazole units are also provided.
专利号:WO-2007141253-A1 优先权日:2006-06-07 标 题 :Process for the production of intermediates for the preparation of tricyclic imidazopyridines 发明人:PALMER ANDREAS; BUHR WILM; ZIMMERMANN PETER JAN; BREHM CHRISTOF; CHIESA MARIA VITTORIA; ZANOTTI-GEROSA ANTONIO 权利人:NYCOMED GMBH; PALMER ANDREAS; BUHR WILM; ZIMMERMANN PETER JAN; BREHM CHRISTOF; CHIESA MARIA VITTORIA; ZANOTTI-GEROSA ANTONIO 摘要:The invention relates to a process for the synthesis of compounds of the formula (1-a) and compounds of the formula (1-b). The compounds of the formula 1-a and the compounds of the formula 1-b, in which the substituents R1, R2, R3, and Arom have the meanings indicated in the description, are valuable intermediates for the preparation of pharmaceutically active compounds.