摘要:
The invention relates to simple and efficient preparation of optically active 7-substituted-2-aminotetralins with industrial advantage. A process for preparation of optically active 7- substituted-2-aminotetralins or salts thereof, which comprises reducing a 7-substituted-2-tetralone or a bisulfite adduct thereof with a microorganism into an optically active 7-substituted-2-tetralol, introducing a sulfonyl group into the hydroxyl group of the tetralol to obtain an optically active 7-substituted-2-sulfonyloxytetralin, introducing a nitrogen substituent into the resulting tetralin by the use of a nitrogen nucleophile through inversion to obtain an optically active 2,7-substituted tetralin, and, if necessary, converting the nitrogen substituent into an unsubstituted amino group.
摘要:
An object of the present invention is to provide a producing method: that allows any hydrophobic peptide to be used as an object to be purified, in hydrophilizing a hydrophobic peptide, synthesized by solid-phase peptide synthesis, with a hydrophilic unit and purifying the hydrophobic peptide by HPLC, regardless of the type of the amino acid residue at the N-terminus; that allows the hydrophilic unit to be flexibly selected in accordance with the type of the hydrophobic peptide; and that is excellent in versatility. The present invention is characterized by a method for producing a purified peptide from a supported crude peptide including a support and a first peptide chain bonded to the support at a C-terminus, the method comprising: a hydrophilization step A of introducing a linker and a hydrophilic unit to an amino group of the supported crude peptide in this order stepwise or at a single step to obtain a support-free hydrophilized peptide; a support cleavage step B of cleaving a bond between the first peptide chain and the support at any stage before bonding the linker to the supported crude peptide until the hydrophilized peptide is obtained, or after a supported hydrophilized peptide is obtained; a chromatographic purification step of treating the support-free hydrophilized peptide obtained by the hydrophilization step A and the support cleavage step B, by liquid chromatography; and a linker cleavage step of cleaving a bond between the linker and the first peptide chain included in the chromatographically-purified support-free hydrophilized peptide, by chemical treatment.
摘要:
An optically active amino acid derivative is prepared either by subjecting an optically active 3-haloalanine derivative (1) to N-protection followed by cyclization or cyclization followed by N-protection to prepare an optically active aziridinecarboxylic acid derivative (3) whose imino group is protected with 2- and/or 4-nitrated benzenesulfonyl and treating this derivative (3) with an organometallic reagent or by subjecting an optically active 3-haloalanine derivative to N-protection to obtain an optically active 3-haloalanine derivative (4) whose amino group is protected with 2- and/or 4-nitrated benzenesulfonyl and treating this derivative (4) with an organometallic reagent. According to such processes, natural and nonnatural optically active amino acids can be prepared from inexpensive raw materials through simple and easy operation. In said derivatives, X is halogen; R?1 and R2¿ are each hydrogen or the like; * represents an asymmetric carbon atom; and P1 is 2- and/ or 4- nitrated benzenesulfonyl.
摘要:
An optically active ketone represented by the following formula (2): wherein, Ar 1 represents a furyl group, a thienyl group or a C 6-20 aryl group; X 1 represents a halogen atom, and * indicates an asymmetric carbon atom, is produced by stereoselectively reducing an enone compound represented by the following formula (1) : wherein, Ar 1 and X 1 represent the same as the above.
摘要翻译:由下式表示的光学活性酮(2):其中,Ar 1表示呋喃基,噻吩基或C 6-20芳基; X 1 darstellt卤原子,和*表示不对称碳原子上,通过立体选择地还原到烯酮由下述式(1)表示的化合物制备:worin中,Ar 1和X 1表示与上述相同。