专利号:US-2023331778-A1 优先权日:2020-08-31 标 题 :An improved process for fmoc synthesis of etelcalcetide 发明人:LOBO LESTER JOHN; CHANDRAKESAN MURALIDHARAN; DOSHI CHETAN; CHANADAK SHAILESH LALCHAND; YADAV NANDLAL GOPAL; MOHE NIKHIL UMESH; VISHWANATHAN KODANDARAMAN; CHAVRE PRAFUL SHAMRAO 权利人:USV PRIVATE LTD 摘要:The present invention relates to an improved process for the synthesis of Etelcalcetide and its analogs by solid phase synthesis of Fmoc protected amino acids in a sequential manner, followed by acetylation of terminal D-cys and cleavage of peptide from solid support. The crude heptapeptide thus obtained is reduced using Tris(2-carboxyethyl) phosphine hydrochloride, purified and oxidized with L-cysteine. The oxidized Etelcalcetide is purified and salt exchanged using a one-step reverse phase chromatography process. The purified Etelcalcetide hydrochloride is then precipitated using organic solvents, concentrated and lyophilized to purity of greater than 99.0%.
专利号:US-7812193-B2 优先权日:2003-09-19 标题:Process for enantioselective synthesis of single enantiomers of modafinil by asymmetric oxidation 发明人:REBIERE FRANCOIS; DURET GERARD; PRAT LAURENCE 权利人:CEPHALON FRANCE 摘要:The invention relates to a method for preparing a sulphoxide compound of formula (I) either as a single enantiomer or in an enantiomerically enriched form, comprising the steps of:n a) contacting a pro-chiral sulphide of formula (II) with a metal chiral complex, a base and an oxidizing agent in an organic solvent; and optionally b) isolating the obtained sulphoxide of formula (I); nn nwherein n, Y, R 1 , R 1a , R 2 and R 2a are as defined herein.
专利号:US-8816050-B2 优先权日:2006-03-22 标题:Method of preparing glycopeptides 发明人:WONG CHI-HUEY; BRIK ASHRAF; YANG YU-YING; FICHT SIMON; PAYNE RICHARD 权利人:WONG CHI-HUEY; BRIK ASHRAF; YANG YU-YING; FICHT SIMON; PAYNE RICHARD; SCRIPPS RESEARCH INST 摘要:A method is provided for the synthesis of glycopeptides using a sugar assisted ligation strategy, wherein an N-terminal peptide portion in the form of a thioester is coopled with a C-terminal peptide portion bearing a carbohydrate moiety comprising a thiol group.
专利号:US-9012648-B2 优先权日:2012-08-21 标题 :Haptens of risperidone and paliperidone 发明人:HASPESLAGH PIETER RIK; VLIEGEN MAARTEN; HRYHORENKO ERIC; DECORY THOMAS R; SANKARAN BANUMATHI 权利人:JANSSEN PHARMACEUTICA NV; ORTHO CLINICAL DIAGNOSTICS INC 摘要:The invention relates to compounds of Formula I, wherein R1 and R2 are defined in the specification, useful for the synthesis of novel conjugates and immunogens derived from risperidone and paliperidone. The invention also relates to conjugates of a risperidone or paliperidone hapten and a protein.
专利号:US-9394354-B2 优先权日:2012-08-21 标题 :Haptens of paliperidone 发明人:HASPESLAGH PIETER RIK; VLIEGEN MAARTEN; HRYHORENKO ERIC; DECORY THOMAS R; SANKARAN BANUMATHI 权利人:JANSSEN PHARMACEUTICA NV; ORTHO CLINICAL DIAGNOSTICS INC 摘要:The invention relates to compounds of Formula I, wherein L 1 , L 2 , and L 3 are defined in the specification, useful for the synthesis of novel conjugates and immunogens derived from paliperidone. The invention also relates to conjugates of a paliperidone hapten and a protein.
专利号:US-9304126-B2 优先权日:2012-08-21 标题:Haptens of quetiapine 发明人:DONAHUE MATTHEW GARRETT; GONG YONG; SALTER RHYS; HRYHORENKO ERIC; DECORY THOMAS R; REMMERIE BART; SANKARAN BANUMATHI 权利人:JANSSEN PHARMACEUTICA NV; ORTHO CLINICAL DIAGNOSTICS INC 摘要:The invention relates to compounds of Formula I, wherein R 1 , R 2 , and R 3 are defined in the specification, useful for the synthesis of novel conjugates and immunogens derived from quetiapine. The invention also relates to conjugates of a quetiapine hapten and a protein.
摘要:Sinha, A. K.; Singh, R., Science of Synthesis, (2021) , 499. 摘要:M. M. Kreevoy, E. T. Harper, R. E. Duvall, H. S. Wilgus and L. T. Ditsch, J. Am. Chem. Soc. 82, 4899 (1960). 摘要:Harris, P. A., Science of Synthesis: Knowledge Updates, (2024) 1, 38.