专利号:US-7173059-B2 优先权日:2003-05-08 标题:Intermediates useful in the synthesis of HIV-protease inhibitors and methods for preparing the same 发明人:ALBIZATI KIM FRANCIS; BABU SRINIVASAN 权利人:AGOURON PHARMA 摘要:Optically active 3-amino-butene and 1,2-dihydroxy-3-amino-butane intermediate compounds, useful in the synthesis of HIV-protease inhibitors and methods of preparing these intermediate compounds are disclosed.
专利号:US-6472534-B2 优先权日:1999-10-21 标 题:Methods for the preparation of intermediates in the synthesis of HIV-protease inhibitors 发明人:BORER BENNETT C; ZOOK SCOTT E; BUSSE JULIETTE K 权利人:AGOURON PHARMA 摘要:Methods for the preparation of chemical intermediates in the synthesis of HIV-protease inhibitors related to and including nelfinavir mesylate are disclosed. The method of this invention comprises converting tetrohydran derivatives into oxazolines to provide key reaction intermediates for the preparation of nelfinavir. Also disclosed is a method for the preparation of a chiral amino alcohol from an epoxy-tetrahydrofuran.
专利号:US-9346851-B2 优先权日:2008-02-22 标 题 :Chemical modification of proteins 发明人:BERNARDES GONCALO; CHALKER JUSTIN; DAVIS BENJAMIN 权利人:BERNARDES GONCALO; CHALKER JUSTIN; DAVIS BENJAMIN; RP SCHERER TECHNOLOGIES LLC 摘要:The invention relates to methods for selectively converting a cysteine residue in a peptide or protein to the dehydroalanine (Dha) residue. The method also works on selenocysteine and substituted cysteine and selenocysteine residues, resulting in the Dha residue which may be converted to any natural or unnatural amino acid residue desired without the alteration of the remainder of the peptide or protein. The invention also allows ligation of a desired peptide at any point rather than at a point where there should be a naturally occurring cysteine, thereby allowing native chemical ligation to be used in the synthesis of peptides that do not contain cysteine. The methodology allows for the synthesis of very large peptides.
专利号:US-4033949-A 优先权日:1976-04-14 标 题:Analogs of thromboxane B2 and processes for their synthesis 发明人:KELLY ROBERT C; NELSON NORMAN A 权利人:UPJOHN CO 摘要:The present specification provides novel intermediates and novel processes for the synthesis of various side chain and skeletal analogs of Thromboxane B 2 (11β-homo-11a-oxa-PGF 2 .sub.α). These analogs are particularly and especially useful as reproductive cycle control agents.
专利号:WO-2014108526-A1 优先权日:2013-01-11 标题 :Synthetic process for the manufacture of pipecolidepsin compounds 发明人:PELAY GIMENO MARTA; GARCà A-RAMOS YESICA; TULLA PUCHE JUDIT; ALBERICIO PALOMERA FERNANDO; MARTà N LÓPEZ M JES S 权利人:PHARMA MAR SA 摘要:(I) wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , R 10 , R 11 , R 12 , n and Y are as described. The invention provides a process for the synthesis of complex pipecolidepsin and related compounds of formula (I), opening a new field of compounds with useful biological properties. The invention also provides intermediates, useful in the synthesis of compounds of formula (I).
专利号:US-2009143426-A1 优先权日:2007-12-04 标 题:Synthesis of 1,3,6-trisubstituted-2-carboxyquinol-4-ones as selective ET A antagonists and their use as medicaments 发明人:STEPHANI RALPH ANTHONY; PATEL HARDIK JITENDRA; REZNIK SANDRA EVE; CANTOR JEROME OWEN 权利人:STEPHANI RALPH ANTHONY; PATEL HARDIK JITENDRA; REZNIK SANDRA EVE; CANTOR JEROME OWEN 摘要:The invention discloses the composition and preparation of various 1,3,6-trisubstituted-2-carboxy-quinol-4-ones of the formula 1 where R is H, alkyl, haloalkyl or hydroxyalkyl, R′ is alkyl, nitro, halogen or NR 2 ′″ where R′″ is alkyl or cycloalkyl, and R″ is H or alkyl. The composition of the invented compounds as methods of antagonizing the action of endothelin-1 to treat cardiovascular, pulmonary diseases and obstetric disorders and preterm labor and preeclampsia in mammals is disclosed.
摘要:Kantchev, E. A. B.; Organ, M. G., Science of Synthesis, (2009) 48, 63. 摘要:Hagen, T. J.; Helgren, T. R., Science of Synthesis Knowledge Updates, (2015) 2, 149. 摘要:Chiba, S.; Narasaka, K., Science of Synthesis Knowledge Updates, (2011) 4, 473. 摘要:Stoltz, B. M.; Mohr, J. T., Science of Synthesis: Stereoselective Synthesis, (2011) 3, 628. 摘要:Le Gall, E., Science of Synthesis: Multicomponent Reactions, (2013) 1, 183.