专利号:US-7429658-B2 优先权日:2003-09-11 标题 :Synthesis of protected pyrrolobenzodiazepines 发明人:HOWARD PHILIP; MASTERSON LUKE 权利人:SPIROGEN LTD 摘要:A method of synthesis of a N-10 protected PBD compound of formula (I): n nvia an intermediate of formula (II) or formula (V):
专利号:US-8557979-B2 优先权日:2004-06-10 标题 :Carbapenem antibacterials with gram-negative activity and processes for their preparation 发明人:CHOI WOO-BAEG; KOWALIK EWA 权利人:CHOI WOO-BAEG; KOWALIK EWA; FOB SYNTHESIS INC 摘要:The present invention provides β-methyl carbapenem compounds and pharmaceutical compositions useful in the treatment of bacterial infections and methods for treating such infections using such compounds and/or compositions. The invention includes administering an effective amount of a carbapenem compound or salt and/or prodrug thereof to a host in need of such a treatment. The present invention is also in the field of synthetic organic chemistry and is specifically provides an improved method of synthesis of β-methyl carbapenems which are useful as antibacterial agents.
专利号:US-4786684-A 优先权日:1986-08-21 标题 :Benzylthioether-linked solid support-bound thiol compounds and method for peptide synthesis 发明人:GLASS JOHN D 权利人:SINAI SCHOOL MEDICINE 摘要:A method for the synthesis of sulfydryl-containing peptides which comprises forming a benzylthioether-linked solid support-bound thiol compound having at least one functional group for generating at least one peptide bond, sequentially coupling at least one protected amino acid or peptide to the compound until a peptide having desired amino acid sequence is obtained, and cleaving the benzylthioether linkage to release the peptide from the support with concomitant regenertion of the sulfydryl group in the peptides. The invention also encompasses compounds having the general formula wherein X is H, NH2, or acyl-NHY, said acyl being an amino acid or a peptide; Y is H, COOH, CONHNH2, the ester COOR1 in which R1 is selected from the group consisting of methyl, ethyl, phenyl, ortho-nitrophenyl and para-nitrophenyl, the amide CONH2, or the amide CONHR2 in which R2 is an amino acid or peptide; and providing that X and Y cannot both be H.
专利号:US-5817758-A 优先权日:1995-06-07 标 题:P-nitrobenzyl side-chain protection for solid-phase synthesis 发明人:LYTTLE MATTHEW H; HOCKER MICHAEL D 权利人:TERRAPIN TECH INC 摘要:Solid phase supported synthesis of peptides and other molecules using protecting groups comprising p-nitrobenzyl is described.
专利号:US-4309346-A 优先权日:1980-03-27 标 题:Process for the preparation of 1-carbapenems and intermediates via trithioorthoacetates 发明人:CHRISTENSEN BURTON G; RATCLIFFE RONALD W; SALZMANN THOMAS N 权利人:MERCK & CO INC 摘要:Disclosed is a process for the total synthesis of 1-carbapenem antibiotics (I) from L-aspartic acid via intermediates II and III: I II III wherein R is hydrogen, a pharmaceutically acceptable ester moiety or salt cation, or a readily removable blocking group; R6 and R7 are, inter alia, independently selected from the group consisting of hydrogen, alkyl, alkenyl, aryl and aralkyl; R1' is hydrogen or a protecting group; and Ra, Rb and Rc are independently selected from alkyl, aryl and aralkyl.
专利号:US-4378315-A 优先权日:1980-05-29 标题:Process for the preparation of thienamycin and intermediates 发明人:CHRISTENSEN BURTON G; RATCLIFFE RONALD W; SALZMANN THOMAS N 权利人:MERCK & CO INC 摘要:Disclosed is a process for the total synthesis of thienamycin from L-aspartic acid via intermediate III: ##STR1## R=H, blocking group or salt cation.