专利号:US-9150498-B2 优先权日:2011-10-25 标题:Process for the preparation of oseltamivir and methyl 3-epi-shikimate 发明人:RAWAT VARUN; DEY SOUMEN; ARUMUGAM SUDALAI 权利人:COUNCIL SCIENT IND RES 摘要:The present invention discloses high yielding enantioselective process for synthesis of Oseltamivir from readily available starting material, cis-1,4-butene diol. The process features incorporation of chirality using sharpless asymmetric epoxidation (AE) and diastereoselective Barbier allylation and construction of cyclohexene carboxylic acid ester core through a ring closing metathesis (RCM) reaction. Further also disclosed herein is synthesis of (−)-methyl 3-epi-shikimate.
专利号:WO-2024262824-A1 优先权日:2023-06-20 标 题 :Novel process for synthesis of polysubstituted pyridine derivatives 发明人:PARK SEUNG BUM; YI SIHYEONG 权利人:SEOUL NAT UNIV R&DB FOUNDATION 摘要:The present invention relates to a novel method for synthesizing a polysubstituted pyridine derivative and, more specifically, to a method for synthesizing a 2,3,5-substituted pyridine derivative through a specific ring cleavage reaction. In the synthesis method of the present invention, an enamine structure is formed in situ by using beta keto ester/sulfone/phosphonic acid ester and ammonium acetate and subjected to an aldol condensation reaction with 3-formyl (aza) indole/benzofuran, a cyclization reaction, and a ring-cleavage reaction in that order to synthesize a characteristic pyridine structure having an alkyl/aryl substituent attached to the 2-position thereof, an ester/sulfone/phosphonic acid ester attached to the 3-position thereof, and ortho-aminoaryl/phenol including various substituents attached to the 5-position thereof. In particular, (aza)indole/benzofuran and beta keto ester/sulfone/phosphonic acid ester, which are reaction substrates, are substrates having very high accessibility, and enable the introduction of various substituents, thereby constructing a pyridine skeleton having high biocompatibility into which ortho-aminoaryl or phenol substituents having various substituents are introduced.
专利号:US-2008242877-A1 优先权日:2007-02-26 标题 :Intermediates and processes for the synthesis of Ramelteon 发明人:KANSAL VINOD KUMAR; MISTRY DHIRENKUMAR N; VASOYA SANJAY L 权利人:KANSAL VINOD KUMAR; MISTRY DHIRENKUMAR N; VASOYA SANJAY L 摘要:Provided are intermediates and processes for preparation of Ramelteon.
专利号:US-6878665-B2 优先权日:2001-09-28 标题:Diphosphines, their complexes with transisition metals and their use in asymmetric synthesis 发明人:DUPRAT DE PAULE SEBASTIEN; CHAMPION NICOLAS; VIDAL VIRGINIE; GENET JEAN-PIERRE; DELLIS PHILIPPE 权利人:SYNKEM 摘要:The invention relates to novel diphosphines, in optically pure or racemic form, of formula (I): n n nin which:n R 1 and R 2 are a (C 5 -C 7 )cycloalkyl group, an optionally substituted phenyl group or a 5-membered heteroaryl group; and A is (CH 2 —CH 2 ) or CF 2 . nn The invention further relates to the use of a compound of formula (I) as a ligand for the preparation of a metal complex useful as a chiral catalyst in asymmetric catalysis, and to the chiral metal catalysts comprising at least one ligand of formula (I).
专利号:US-4145510-A 优先权日:1976-06-21 标 题:5-Substituted phosphonate hydantoins and derivatives thereof 发明人:HALL LUTHER A R; GORDON DAVID A 权利人:CIBA GEIGY CORP 摘要:Hydantoins of the formula wherein R1 is hydrogen or alkyl of 1 to 8 carbon atoms, R2 is R3 is alkyl of 1 to 8 carbon atoms, and X is a straight or branched chain alkylene of 1 to 4 carbon atoms or a straight or branched chain alkylene of 3 to 6 carbon atoms containing an internal carbamido group; or R1 and R2 together are Y where Y is a straight or branched chain alkylene of 4 to 8 carbon atoms having a pendant ARE PREPARED BY REACTING FIRST alpha , beta -UNSATURATED ALDEHYDES OR KETONES WITH ALKYL PHOSPHITES TO FORM A PHOSPHONATE ALDEHYDE OR KETONE FOLLOWED BY A CLASSICAL Bucherer hydantoin synthesis.
专利号:US-8030466-B2 优先权日:2009-09-29 标 题:3′-o-fluorescently modified nucleotides and uses thereof 发明人:SHIN DONGYUN; AHN DAE-RO; AHN HE-CHUL 权利人:KOREA INST SCI & TECH 摘要:The present invention relates to a DNA sequencing method using a nucleoside triphosphate with a fluorescent blocking group on its 3′-OH end as a reversible terminator. Further, the present invention relates to sequencing-by-synthesis method using the mono-modified reversible terminator (MRT), the novel nucleotide monomer having a reversible fluorescent blocking group removable chemically or enzymatically at its 3′-OH end. The sequencing method of the present invention facilitates sequencing of bases inserted by terminating extension of a nucleotide chain by the nucleotide monomer and then detecting fluorescence signal from 3′-OH end. At this time, after analyzing the fluorescence signal, the blocking group conjugated to the 3′-OH end can be effectively removed, indicating that a free 3′-OH functional group can be successfully restored, so that the next monomer insertion is possible, making continuous sequencing possible.