专利号:US-9643915-B2 优先权日:2013-03-15 标题:Methods for the synthesis of sphingomyelins and dihydrosphingomyelins 发明人:ONICIU DANIELA CARMEN; HECKHOFF STEFAN; OSWALD BENOIT; REBMANN PETER; PEER ANDREAS; GONZALEZ MIGUEL; SAUTER PATRIK 权利人:CERENIS THERAPEUTICS HOLDING SA 摘要:The present invention includes methods for the synthesis of sphingomyelins and dihydrosphingomyelins. The present invention also includes methods for the synthesis of sphingosines and dihydrosphingosines. The present invention further includes methods for the synthesis of ceramides and dihydroceramides.
专利号:US-8933181-B2 优先权日:2006-10-06 标题:Branched polymers and methods for their synthesis and use 发明人:MOURI HIROSHI; LUO STEVEN; KURASCH JESSICA; ROBERTSON CHRISTOPHER G; WARREN SANDRA 权利人:MOURI HIROSHI; LUO STEVEN; KURASCH JESSICA; ROBERTSON CHRISTOPHER G; WARREN SANDRA; BRIDGESTONE CORP 摘要:Branched polymers including multi-branched polymers, functionalized branched polymers, star-branched polymers, and dendigraft polymers. Methods for the synthesis of branched polymers and method for the use of branched polymers in tire components are also included.
专利号:US-4331688-A 优先权日:1978-02-23 标题 :Therapeutic method for inhibiting gastric secretion by administration of 15-deoxy-16-hydroxy prostaglandins 发明人:KLUENDER HAROLD C; WOESSNER WARREN D; BIDDLECOM WILLIAM G 权利人:MILES LAB 摘要:Analogues of PGE 1 having the structural formula, ##STR1## in which J is R-hydroxymethylene or S-hydroxymethylene; R 1 is hydrogen; R 2 is hydrogen or together with R 4 is a methylene chain of 2 to 3 carbon atoms such that a cycloalkyl of 5 to 6 carbon atoms inclusive is formed; R 3 is hydrogen or methyl, or together with R 4 is a methylene or a lower alkylated methylene chain of 2 to 5 carbon atoms such that a cycloalkyl or a lower alkylated cycloalkyl of 4 to 7 carbon atoms inclusive is formed, or together with R 4 is bicycloalkyl or bicycloalkenyl moiety having the formula: ##STR2## such that a bicycloalkyl or bicycloalkenyl compound is formed, wherein m and n are integers having a value from 0 to 3, p is an integer having a value from 0 to 4 and q is an integer having a value of from 1 to 4 and wherein the double bond of such bicycloalkenyl is in the m, n, p, or q bridge; R 4 is hydrogen or methyl or together with R 2 or R 3 forms a cycloalkyl or bicycloalkyl or bicycloalkenyl as defined above, or together with R 5 is a methylene chain of 3 to 5 carbon atoms such that a cycloalkyl of 4 to 6 carbon atoms inclusive is formed; R 5 is selected from the group consisting of hydrogen, straight-chain alkyl having from 1 to 3 carbon atoms or together with R 4 forms a cycloalkyl as defined above; and R 6 is hydrogen or straight-chain alkyl having from 1 to 3 carbon atoms are disclosed. n PGE 1 ester analogues of the above formula, limited to the structures wherein two of R 2 , R 3 R 4 and R 5 form a cycloalkyl, lower alkylated cycloalkyl, bicycloalkyl or bicycloalkenyl are also disclosed. n The prostaglandin analogues selectively produce bronchodilation and decrease gastric secretion in vivo. n Methods of preparing the analogues and starting materials required in the synthesis of the analogues are also disclosed.
专利号:US-4132738-A 优先权日:1978-02-23 标 题:Preparation of 15-deoxy-16-hydroxyprostaglandins 发明人:KLUENDER HAROLD C; WOESSNER WARREN D; BIDDLECOM WILLIAM G 权利人:MILES LAB 摘要:Analogues of PGE 1 having the structural formula, ##STR1## in which J is R-hydroxymethylene or S-hydroxymethylene; R 1 is hydrogen; R 2 is hydrogen or together with R 4 is a methylene chain of 2 to 3 carbon atoms such that a cycloalkyl of 5 to 6 carbon atoms inclusive is formed; R 3 is hydrogen or methyl, or together with R 4 is a methylene or a lower alkylated methylene chain of 2 to 5 carbon atoms such that a cycloalkyl or a lower alkylated cycloalkyl of 4 to 7 carbon atoms inclusive is formed, or together with R 4 is bicycloalkyl or bicycloalkenyl moiety having the formula: ##STR2## SUCH THAT A BICYCLOALKYL OR BICYCLOALKENYL COMPOUND IS FORMED, WHEREIN M AND N ARE INTEGERS HAVING A VALUE FROM 0 TO 3, P IS AN INTEGER HAVING A VALUE FROM 0 TO 4 AND Q IS AN INTEGER HAVING A VALUE OF FROM 1 TO 4 AND WHEREIN THE DOUBLE BOND OF SUCH BICYCLOALKENYL IS IN THE M, N, P, OR Q BRIDGE; R 4 is hydrogen or methyl or together with R 2 or R 3 forms a cycloalkyl or bicycloalkyl or bicycloalkenyl as defined above, or together with R 5 is a methylene chain of 3 to 5 carbon atoms such that a cycloalkyl of 4 to 6 carbon atoms inclusive is formed; R 5 is selected from the group consisting of hydrogen, straight-chain alkyl having from 1 to 3 carbon atoms or together with R 4 forms a cycloalkyl as defined above; and R 6 is hydrogen or straight-chain alkyl having from 1 to 3 carbon atoms are disclosed. n Pge 1 ester analogues of the above formula, limited to the structures wherein two of R 2 , R 3 R 4 and R 5 form a cycloalkyl, lower alkylated cycloalkyl, bicycloalkyl or bicycloalkenyl are also disclosed. n The prostaglandin analogues selectively produce bronchodilation and decrease gastric secretion in vivo. n Methods of preparing the analogues and starting materials required in the synthesis of the analogues are also disclosed.
专利号:WO-2013046211-A1 优先权日:2011-09-27 标 题 :Processes for the preparation of 5-chloro-n-({(5s)-2-oxo-3-[4-(3-oxo-4-morpholinyl) phenyl]-1,3-oxazolidin-5-yl}methyl)-2-thiophene-carboxamide and intermediates thereof 发明人:MOHAN RAO DODDA; KRISHNA REDDY PINGILI; VENKAT REDDY BUTHUKURI 权利人:SYMED LABS LTD; MOHAN RAO DODDA; KRISHNA REDDY PINGILI; VENKAT REDDY BUTHUKURI 摘要:TThe present invention provides processes for the preparation of 5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)phenyl]-1,3-oxazolidin-5-yl}methyl)-2-thiophene-carboxamide (I) and intermediates thereof. Also provides novel intermediates and their use in the synthesis of oxazolidine derivatives.
专利号:US-6448449-B2 优先权日:2000-04-21 标题:Process for preparation of (R)-1- (aryloxy)propan-2-ol 发明人:LARROW JAY FRANCIS 权利人:RHODIA CHIREX INC 摘要:A process for the preparation of (R)-1-(2,3-difluoro-6-nitrophenoxy)-propan-2-ol, which is a useful intermediate in the synthesis of the widely used antibiotic Levofloxacin is provided. A process for the preparation of (R)-1-(2,3-difluoro-6-nitrophenoxy)-2-trimethylsiloxypropane is also described. The process includes the ring opening of (R)-propylene oxide with 2,3-difluoro-6-nitrophenyl trimethylsilyl ether in the presence of an optically active Co(salen) catalyst. The trimethylsilyl group of the reactant is transferred to the product aryloxy alcohol, which serves to protect the secondary alcohol in situ. Upon isolation, the trimethylsilyl group is removed and the resulting regioisomeric mixture purified to yield the desired (R)-1-(2,3-difluoro-6-nitrophenoxy)-propan-2-ol in high purity and yield.
[参考文献]: Salvatore Debonis, Et Al. Structure-Activity Relationship Of S-Trityl-L-Cysteine Analogues As Inhibitors Of The Human Mitotic Kinesin Eg5. J Med Chem. 2008 Mar 13;51(5):1115-25.
合成参考文献
摘要:U.S. Army Armament Research & Development Command, Chemical Systems Laboratory, NIOSH Exchange Chemicals., NX#04015 摘要:Kitching, W.; Glenn, M., Science of Synthesis, (2004) 3, 189. 摘要:Spivey, A. C.; Diaper, C. M., Science of Synthesis, (2003) 5, 146. 摘要:Chen, G., Science of Synthesis, (2005) 6, 94. 摘要:Kitching, W.; Glenn, M., Science of Synthesis, (2004) 3, 271.