专利号:US-3992413-A 优先权日:1975-07-25 标 题 :Intermediates in the synthesis of prostaglandins 发明人:TAUB DAVID; WENDLER NORMAN L 权利人:MERCK & CO INC 摘要:The invention relates to a new and novel synthesis of prostaglandin E 2 , and it particularly relates to a novel process starting with relatively inexpensive starting materials. The invention further relates to a synthesis which is readily adaptable for large scale processing because of the high yields in the individual reaction steps. n The invention further relates to novel compounds formed as intermediates in the synthesis of prostaglandin E 2 . The invention still further relates to synthetic analogs and known metabolites of prostaglandin E 2 and prostaglandin E 1 , useful as standards in certain biological assays for determining prostaglandin-like activity.
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-9708354-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-4870199-A 优先权日:1986-04-30 标题 :Processes for the synthesis of diprotected R[R*,S*]-3,5-dihydroxy-6-oxohexanoate esters 发明人:CHEN KAU-MING; HARDTMANN GOETZ E; KAPA PRASAD K; LEE GEORGE T; LINDER JEROME; WATTANASIN SOMPONG 权利人:SANDOZ PHARMACEUTICALS CORP 摘要:Process for the synthesis of compounds of the formula in R[R*,S*] enantiomeric form, wherein each P1 is independently an hydroxy group-protecting group, and R2z is C1-4alkyl, benzyl or allyl, comprising, as a key step when R2z is R2x, the reaction of the compound of the formula in (S) enantiomeric form with a compound of the formula Mg &cir& +2 ((-)OOC-CH2-COOR2x)2 to obtain a compound of the formula in (S) enantiomeric form, and, as a key step when R2z is R2y, the reaction of a compound of the formula in (S) enantioimeric form with a compound of the formula Li(+)(-)CH2-COOR2y to obtain a compound of the formula in (S) enantiomeric form, wherein R2x is primary or secondary C1-4alkyl, benzyl or allyl, R2y is C1-4alkyl not containing an asymmetric carbon atom, and R3' is methyl or ethyl, processes for the synthesis of compounds of the formula comprising reacting a compound of the formula with the reaction product of a strong base and a compound of the formula optionally followed by, when R2z is allyl, cleavage of the allyl and P1 groups to obtain the corresponding compound of the formula wherein each R7 is methyl or ethyl, R is as defined in the specification, and each P1 independently and R2z are as defined above, and the compounds of the formula wherein R and each R7 are as defined above.
专利号:US-9783549-B2 优先权日:2013-11-04 标题:Macrocyclization reactions and intermediates useful in the synthesis of analogs of halichondrin B 发明人:FANG FRANCIS G; KIM DAE-SHIK; CHOI HYEONG-WOOK; CHASE CHARLES E; LEE JAEMOON 权利人:EISAI R&D MAN CO LTD 摘要:The invention provides methods for the synthesis of eribulin or a pharmaceutically acceptable salt thereof (e.g., eribulin mesylate) through a macrocyclization strategy. The macrocyclization strategy of the present invention involves subjecting a non-macrocyclic intermediate to a carbon-carbon bond-forming reaction (e.g., an olefination reaction (e.g., Homer-Wadsworth-Emmons olefination), Dieckmann reaction, catalytic Ring-Closing Olefin Metathesis, or Nozaki-Hiyama-Kishi reaction) to afford a macrocyclic intermediate. The invention also provides compounds useful as intermediates in the synthesis of eribulin or a pharmaceutically acceptable salt thereof and methods for preparing the same.
专利号:US-5703223-A 优先权日:1994-09-02 标题 :Solid phase synthesis of oligonucleotides with stereospecific substituted phosphonate linkages by pentavalent grignard coupling 发明人:WICKSTROM ERIC; LE BEC CHRISTINE 权利人:UNIV JEFFERSON 摘要:The present invention provides a method for producing an oligonucleotide having stereospecific substituted phosphonate linkages by use of a pentavalent Grignard coupling reaction on a solid phase support. The method can be used for automated synthesis of oligonucleotides having sequential equatorial or axial stereospecific substituted phosphonate linkages.
参考文献:10.1166/jnn.2011.4193 摘要:Wang Y, Wang Z, Hu N, Wei L, Xu D, Wei H, Kong ES, Zhang Y. Hexafluorobisphenol A covalently functionalized single-walled carbon nanotubes for detection of dimethyl methylphosphonate vapor. J Nanosci Nanotechnol. 2011 Jun;11(6):4874–81. doi: 10.1166/jnn.2011.4193.