摘要:
A method for the reduction of an allyl alcohol-type compound specific to its allylic hydroxyl group, which is carried out without any side reactions, such as reduction of other parts of the compound and allylic rearrangement, which method comprises treating said compound with a trialkylsilane in the presence of A1X₃, wherein X is a halogen atom.
摘要:
A process for preparing an optically active compound useful as an intermediate for the preparation of clinically important thromboxane A₂ (TXA₂) receptor antagonist by resolving a racemic mixture of norbornyl amine of formula (I):
wherein R¹ is hydrogen, lower alkyl or lower alkyl substituted with -COOR³ at the terminal methyl residue; R³ is lower alkyl; Y is oxygen or methylene; m and n are independently 0 or 1 with a chiral acid.
摘要翻译:通过拆分式(I)的降冰片基胺的外消旋混合物制备用作制备临床上重要的血栓素A2(TXA2)受体拮抗剂的中间体的光学活性化合物的方法:其中R 1为氢, 在末端甲基残基上被-COOR 3取代的低级烷基或低级烷基; R 3是低级烷基; Y是氧或亚甲基; m和n与手性酸独立地为0或1。
摘要:
A process for preparing an optically active compound useful as an intermediate for the preparation of clinically important thromboxane A₂ (TXA₂) receptor antagonist by resolving a racemic mixture of norbornyl amine of formula (I):
wherein R¹ is hydrogen, lower alkyl or lower alkyl substituted with -COOR³ at the terminal methyl residue; R³ is lower alkyl; Y is oxygen or methylene; m and n are independently 0 or 1 with a chiral acid.
摘要翻译:通过拆分式(I)的降冰片基胺的外消旋混合物制备用作制备临床上重要的血栓素A2(TXA2)受体拮抗剂的中间体的光学活性化合物的方法:其中R 1为氢, 在末端甲基残基上被-COOR 3取代的低级烷基或低级烷基; R 3是低级烷基; Y是氧或亚甲基; m和n与手性酸独立地为0或1。
摘要:
Pharmaceutical or veterinary preparations for use in the treatment of thromboxane A₂ mediating diseases, comprising a pharmacologically effective amount of at least one compound of the formula: wherein R¹ is carboxyl or 5-tetrazolyl, R² is hydrogen, methyl, hydroxy, chloro, or bromo, or a pharmaceutically acceptable ester or salt thereof, formulated for such use with one or more non-toxic pharmaceutically or veterinarily acceptable carrier and optionally in unit dosage form.
摘要:
The invention provides optically active esters of arylacetic acid of the formula: wherein R¹ is hydrogen or optionally substituted C₁-C₂ alkyl or phenyl or when both taken together form C₂-C₆ alkylene, C₂ or C₄-C₆ alkenylene, or a bicyclic-ring; R² is hydrogen or methyl; X is a single bond or CH₂, C=O, N-R⁴, O, S, CHNHR⁴, CHCH₃, CH-Ar, or CHOR⁵ (provided that when X is single bond or CH₂, C=O, N-R⁴, O, or S, R¹ and R² are not simultaneously hydrogen or methyl); R³ is hydrogen, optionally substituted alkyl, or optionally substituted aralkyl; R⁴ is hydrogen or an amino protecting group; R⁵ is hydrogen or a hydroxy protecting group; and Ar is optionally substituted aryl. These esters may be prepared by the reaction of a σ symmetric acid anhydride with an (R)- or (S)-arylacetic acid derivative in high optical purity, and are useful as intermediates for various optically active natural products and medicines.