专利号:WO-0110798-A1 优先权日:1999-08-04 标题 :Solid phase synthesis of oxa- and thiazoles 发明人:BUNIN BARRY A; TUSHUP STEVEN P 权利人:CHEMRX ADVANCED TECHNOLOGIES I; BUNIN BARRY A; TUSHUP STEVEN P 摘要:Thia- and oxazole-4-carboxylic acid derivatives are prepared by solid phase synthesis, using intermediates of formula (α) where SS is a solid support and n is 0 or 1.
专利号:WO-2024129887-A1 优先权日:2022-12-13 标题:Biobased synthesis of glucodiamine 发明人:MILLET AGUSTIN; WOELK HANS-JOERG; LEE TONI M; CHAKRABARTI GAURAB; HUNT SEAN 权利人:SOLUGEN INC 摘要:A method of preparing glucodiamine, comprising contacting glucose with an enzyme oxidation catalyst under conditions suitable for the formation of glucodialdose; contacting glucodialdose with a nitrogen-containing compound under conditions suitable for the formation of glucodioxime; and reducing glucodioxime under conditions suitable for the formation of glucodiamine. A method of preparing glucodiamine, comprising contacting glucodioxime with a dehydration catalyst under conditions suitable for the formation of glucodinitrile; and reducing glucodinitrile under conditions suitable for the formation of glucodiamine. A chemoenzymatic method of producing a bio-based amide platform chemical, comprising: contacting glucose with a biocatalyst under conditions suitable for the formation of glucodialdose; contacting glucodialdose with a base under conditions suitable for the formation of glucodioxime; and contacting glucodioxime with a hydrogenation catalyst in the presence of hydrogen under conditions suitable for formation of glucodiamine.
专利号:WO-0127095-A1 优先权日:1999-10-14 标 题:Method for producing 2-(n-boc-aminomethyl)-thiazol-4-carboxylic acid 发明人:BUSCHMANN ERNST; PFEIFFER THOMAS 权利人:BASF AG; BUSCHMANN ERNST; PFEIFFER THOMAS 摘要:The synthesis of dolastatin 3, which inhibits cell growth, requires a 2-aminomethyl-thiazol-4-carboxylic acid that is protected on the amino group as a building block. The invention provides a synthesis for producing this compound with a high degree of purity and a high yield so that it is also feasible on an industrial scale. To this end, a glycine thioamide with a protective group on the amino group is reacted preferably with 3-brom-2-oxo-propionic acid in the presence of at least one tertiary amine.
专利号:US-2018147294-A1 优先权日:2013-06-06 标 题:Antibody-drug conjugates, compositions and methods of use 发明人:JACKSON DAVID Y; HA EDWARD; PROBST GARY D 权利人:JACKSON DAVID Y; HA EDWARD; PROBST GARY D 摘要:Antibody-cytotoxin antibody-drug conjugates and related compounds, such as linker-cytotoxin conjugates and the linkers used to make them, tubulysin analogs, and intermediates in their synthesis; compositions; and methods, including methods of treating cancers.
专利号:US-10308595-B2 优先权日:2013-02-15 标 题:Albicidin derivatives, their use and synthesis 发明人:SUESSMUTH RODERICH; KRETZ JULIAN; SCHUBERT VIVIEN; PESIC ALEXANDER; HUEGELLAND MANUELA; ROYER MONIQUE; COCIANCICH STEPHANE; ROTT PHILIPPE; KERWAT DENNIS; GRAETZ STEFAN 权利人:UNIV BERLIN TECH 摘要:Antibiotically active compounds characterized by general formula (I), wherein X1, BB, BC, BD, BE and X2 are building blocks with D1, D2, D3, D4 or D5 being linkers which include carbon, sulphur, nitrogen, phosphor and/or oxygen atoms and which are covalently connecting the moities BA and BB, BB and BC, BC and BD, BD and BE and BE and BF, respectively, and wherein in particular the building block BC comprises an amino acid derivative. The compounds for use in a method of treatment of diseases, in particular for use in a method of treatment of bacterial infections are also disclosed.
专利号:EP-4634396-A1 优先权日:2022-12-13 标 题:Biobased synthesis of glucodiamine