专利号:EP-3617181-A1 优先权日:2018-08-30 标题:Synthesis of trans-2-phenylcyclopropylamine or a salt or solvate thereof 发明人:BREUNING ALEXANDER; LIMMERT MICHAEL; DELLING AXEL; HOFMEIER HARALD; HULTSCH JANA; MICKSCH MAIK; SOMMER CHRISTIAN 权利人:AREVIPHARMA GMBH 摘要:The present invention relates to the field of manufacturing trans-2-phenylcyclopropylamine or a salt or solvate thereof, in particular in the form of the sulphate salt. The obtained product, particularly when in the form of the synthesis of trans-2-phenylcyclopropylamine sulphate, is exceptionally pure, substantially free from reactants and reagents that are mutagenic, hazardous or of great concern to the health of humans or the environment.
专利号:US-8987504-B2 优先权日:2010-06-18 标题 :Aminohydroxylation of alkenes 发明人:MEE SIMON PETER HAROLD; LUXENBURGER ANDREAS; HARRIS LAWRENCE DANIEL 权利人:MEE SIMON PETER HAROLD; LUXENBURGER ANDREAS; HARRIS LAWRENCE DANIEL; VICTORIA LINK LTD 摘要:The invention relates to a process for the aminohydroxylation of alkenes using N-oxycarbamate reagents, e.g. N-acyloxycarbamate, N-alkyloxycarbonyloxycarbamate and N-aralkoxycarbonyloxycarbamate reagents. The invention particularly relates to an intermolecular aminohydroxylation reaction that can be carried out in the absence of added base. The invention also relates to novel N-oxycarbamate reagents that are stable crystalline materials. The process of the invention is useful in the synthesis of compounds having a vicinal amino alcohol moiety, such as biologically active compounds.
专利号:US-6509506-B1 优先权日:1997-05-21 标 题 :Two step synthesis of D- and L- α-amino acids and D- and L- α-amino aldehydes 发明人:SHARPLESS K BARRY; LI GUIGEN 权利人:SCRIPPS RESEARCH INST 摘要:D- and L- α-amino acids and D- and L-α-amino aldehydes are synthesized from olefin substrates in two steps. The first step is a catalyzed asymmetric aminohydroxylation addition reaction to the olefin substrate. The addition reaction is catalyzed by osmium and is co-catalyzed by chiral ligands. The chiral ligands, in addition to being co-catalysts with the osmium, also serve to direct the addition reaction regioselectively and enantioselectively, divalent ligands are preferred over monovalent ligands because of their enhanced regio-and enantio-selectivity. As an oxidant nitrogen source for the addition reaction, either a carbamate or sulfonamide may be employed. If carbamate is employed as an oxidant nitrogen source, the resultant β-hydoxycarbamate is deprotected to yield the corresponding β-hydroxyamine. If sulfonamide is employed as an oxidant nitrogen source, the resultant β-hydroxysulfonamide is deprotected to yield the corresponding β-hydroxyamine. The resultant β-hydroxyamine is then selectively oxidized in a second synthetic step to produce the desired D- and L- α-amino acid or D- and L-α-amino aldehyde.
专利号:US-5994583-A 优先权日:1996-05-22 标 题 :Two step synthesis of D- and L- α-amino acids and D- and L- α-amino-aldehydes 发明人:SHARPLESS K BARRY; LI GUIGEN 权利人:SCRIPPS RESEARCH INST 摘要:D- and L-α-amino acids and D- and L-α-amino aldehydes are synthesized from olefin substrates in two steps. The first step is a catalyzed asymmetric aminohydroxylation addition reaction to the olefin substrate. The addition reaction is catalyzed by osmium and is co-catalyzed by chiral ligands. The chiral ligands, in addition to being co-catalysts with the osmium, also serve to direct the addition reaction regioselectively and enantioselectively. Divalent ligands are preferred over monovalent ligands because of their enhance regio- and enantio-selectivity. As an oxidant nitrogen source for the addition reaction, either a carbamate or sulfonamide may be employed. If carbamate is employed as an oxidant nitrogen source, the resultant β-hydroxycarbamate is deprotected to yield the corresponding β-hydroxyamine. If sulfonamide is employed as an oxidant nitrogen source, the resultant β-hydroxysulfonamide is deprotected to yield the corresponding β-hydroxyamine. The resultant β-hydroxyamine is then selectively oxidized in a second synthetic step to produce the desired D- and L-α-amino acid or D- and L-α-amino aldehyde.
专利号:WO-9744312-A1 优先权日:1996-05-22 标题:TWO STEP SYNTHESIS OF D- AND L- α-AMINO ACIDS AND D- AND L- α-AMINO ALDEHYDES
专利号:CN-101029049-B 优先权日:2007-03-23 标题:Application of recyclable and reusable cinchona alkaloid derivative ligands in the synthesis of paclitaxel and docetaxel side chains