CAS: 565-71-9; Dl-Isoserine

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专利信息

专利号:WO-2013138200-A1
优先权日:2012-03-13
标 题 :Green chemistry synthesis of the malaria drug amodiaquine and analogs thereof
发明人：FORTUNAK JOSEPH MARIAN; KULKARNI AMOL ANANT; KING CHRISTOPHER
权利人:UNIV HOWARD
摘要:Methods are provided for a green chemistry one-pot synthesis of amodiaquine and amodiaquine analogs. The methods have a lower environmental impact, lower investment cost, reduced amounts of byproducts and impurities, and a shorter synthesis time, compared to current conventional synthesis methods. The methods reduce the total number of steps in the synthesis from four to five down to two, thereby simplifying production; and allow a reduced number of solvents and reagents to be used in production, thereby reducing the waste generated in the synthesis. The methods can reduce the waste to about 3-5 kilograms of waste generated per kilogram of product produced; and surprisingly improve the overall yield from 60-65% to greater than 90% as compared to the current conventional synthesis methods for amodiaquine and its analogs.

专利号:US-2024409495-A1
优先权日:2021-10-20
标 题 :Process for the preparation of 2,7-dihydroxy-9-fluorenone useful for the synthesis of tilorone and its salts
发明人：JAISANKAR PARASURAMAN; DEB INDUBHUSAN; BHATTACHARJEE PINAKI
权利人:COUNCIL SCIENT IND RES
摘要:Methods involving preparation of building blocks of 2,7-dihydroxy-9-fluorenone toward the synthesis of tilorone dihydrochloride salt and other salts (bromide, iodide, fluoride, citrate, oxalate, maleate, phosphate, tartrate, triflate, trifluoroacetate, tetrafluoroborate) of tilorone, and an efficient, safe, cost effective method for the preparation of 2,7-bis-[2-(diethylamino)ethoxy]-fluorenone-9 and its various salts are developed. The methods involve oxygenation of fluorene, nitration of fluorenone, followed by reduction and diazotization toward the formation of 2,7-dihydroxy-9-fluorenone, which is the key intermediate for the formation of 2,7-bis-[2-(diethylamino)ethoxy]-9-fluorenone-dihydrochloride (Tilorone dihydrochloride) and other tilorone salts. The synthesis method has relatively simple operation, mild reaction conditions, high yield, and simple process with yields of 80-97%. Subsequent product purification of this method uses filtration and crystallization methods, avoiding the existing methods of column chromatography. Therefore, the research of its synthetic method being with a wide range of applications from the drug development and material synthesis point of view.

专利号:US-7452994-B2
优先权日:2001-09-12
标 题 :Synthesis of enantiomerically pure amino-substituted fused bicyclic rings
发明人：MCEACHERN ERNEST J; BRIDGER GARY J; SKUPINSKA KRYSTYNA A; SKERLJ RENATO T; YANG WEN
权利人:ANORMED INC
摘要:This invention describes various processes for synthesis and resolution of racemic amino-substituted fused bicyclic ring systems. One process utilizes selective hydrogenation of an amino-substituted fused bicyclic aromatic ring system. An alternative process prepares the racemic amino-substituted fused bicyclic ring system via nitrosation. In addition, the present invention describes the enzymatic resolution of a racemic mixture to produce the (R)- and (S)-forms of amino-substituted fused bicyclic rings as well as a racemization process to recycle the unpreferred enantioner. Further provided by this invention is an asymmetric synthesis of the (R)- or (S)-enantiomer of primary amino-substituted fused bicyclic ring systems.

专利号:US-5574176-A
优先权日:1995-04-26
标题:Synthesis of an intermediate for the preparation of 5,6-dihydro-(s)-4-(ethylamino)-(s)-6-methyl-4h-thieno [2,3-b]thiopyran-2-sulfonamide 7,7-dioxide intermediates and related compounds
发明人：MATHRE DAVID J; SOHAR PAUL; BROWN LYNN M
权利人:MERCK & CO INC
摘要:This invention is concerned with an improved process for the synthesis of and intermediate en route to 5,6-dihydro-(s)-4-(ethylamino)-(s)-6-methyl-4h-thieno[2,3-b]thiopyran-2-sulfonamide 7,7-dioxide and related compounds. The instant process reduces the reaction time for the synthesis of the key intermediate from 3 to 4 days to from about 2 to about 4 hours while retaining the high enantiomeric purity of the product.

专利号:US-6951932-B2
优先权日:2001-10-25
标 题:Synthesis of 2-aralkoxyadenosines and 2-alkoxyadenosines
发明人：MOORMAN ALLAN R
权利人:KING PHARMACEUTICALS RES & DEV
摘要:The invention provides new methods for synthesis of 2-aralkyloxyadenosines and 2-alkoxyadenosines. The invention is particularly useful for synthesis of 2-[2-(4-chlorophenyl)ethoxy]adenosine. Preferred methods of the invention include activating a guanosine compound followed by hydrolysis; alkylating the hydrolyzed compound with subsequent animation to provide a 2-aralkyloxyadenosine or a 2-alkoxyadenosine compound.

专利号:US-2011130591-A1
优先权日:2009-06-03
标 题:Steroselective synthesis of certain trifluoromethyl-substituted alcohols
发明人：FANDRICK DANIEL R; REEVES JONATHAN T; SONG JINHUA J
权利人:BOEHRINGER INGELHEIM INT
摘要:A process for synthesis of a compound of Formula (X) n n n n n n n n n n wherein:n R 1 is an aryl group substituted with one to three substituent groups,n wherein each substituent group of R 1 is independently C 1 -C 5 alkyl, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, halogen, carboxy, cyano, or trifluoromethyl,n wherein each substituent group of R 1 is optionally independently substituted with one to three substituents selected from C 1 -C 3 alkyl, C 1 -C 3 alkoxy, phenyl, and alkoxyphenyl; and n n R 2 and R 3 are each independently C 1 -C 5 alkyl.