摘要:
Substantially optically pure (S)-trans-{4-[({2-[({1-[3,5-bis(trifluoromethyl)phenyl]ethyl}{5-[2-(methylsulfonyl)ethoxy]pyrimidin-2-yl}amino)methyl]-4-(trifluoromethyl)phenyl}(ethyl)amino)methyl]cyclohexyl}acetic acid, or a salt thereof, or a solvate thereof, which has actions of reducing amount of PCSK9 protein and increasing amount of LDL receptor.
摘要:
Substantially optically pure (S)-trans-{4-[({2-[({1-[3,5-bis(trifluoromethyl)phenyl]ethyl}{5-[2-(methylsulfonyl)ethoxy]pyrimidin-2-yl}amino)methyl]-4-(trifluoromethyl)phenyl}(ethyl)amino)methyl]cyclohexyl}acetic acid, or a salt thereof, or a solvate thereof, which has actions of reducing amount of PCSK9 protein and increasing amount of LDL receptor.
摘要:
A method for preparing optically active 1-bromo-1-[3,5-bis(trifluoromethyl)-phenyl]ethane having a high optical purity, which comprises the step of brominating optically active 1-[3,5-bis(trifluoromethyl)phenyl]ethanol by using, as a brominating agent, (a) a combination of a phosphorus halide and hydrogen bromide, (b) a combination of 1,2-dibromo-1,1,2,2-tetrachloroethane and an organic phosphorous compound represented by the general formula (I): P(R1)(R2)(R3) (in the formula, R1, R2, and R3 independently represent a C6-10 aryl group, a C6-10 aryloxy group, a C1-10 alkyl group, a C1-10 alkoxyl group, a C3-6 cycloalkyl group, or a C3-6 cycloalkoxy group), or (c) a combination of N-bromosuccinimide and a dialkyl sulfide.
摘要:
A method for preparing optically active 1-bromo-1-[3,5-bis(trifluoromethyl)-phenyl]ethane having a high optical purity, which comprises the step of brominating optically active 1-[3,5-bis(trifluoromethyl)phenyl]ethanol by using, as a brominating agent, (a) a combination of a phosphorus halide and hydrogen bromide, (b) a combination of 1,2-dibromo-1,1,2,2-tetrachloroethane and an organic phosphorous compound represented by the general formula (I): P(R1)(R2)(R3) (in the formula, R1, R2, and R3 independently represent a C6-10 aryl group, a C6-10 aryloxy group, a C1-10 alkyl group, a C1-10 alkoxyl group, a C3-6 cycloalkyl group, or a C3-6 cycloalkoxy group), or (c) a combination of N-bromosuccinimide and a dialkyl sulfide.
摘要:
A method for preparing a trans-{4-[(alkylamino)methyl]cyclohexyl}acetic acid, which is useful as a raw material compound for manufacture of medicaments and the like, comprising the step of reducing amide group of a compound represented by the following general formula (6) (R1 represents hydrogen atom or a C1-6 alkyl group, and R2 represents a C1-6 alkyl group, a C3-6 cycloalkyl group, a (C3-6 cycloalkyl)(C1-6 alkyl) group, a C6-10 aryl group, or a C7-12 aralkyl group).
摘要:
A method for preparing a trans-{4-[(alkylamino)methyl]cyclohexyl}acetic acid, which is useful as a raw material compound for manufacture of medicaments and the like, comprising the step of reducing amide group of a compound represented by the following general formula (6) (R1 represents hydrogen atom or a C1-6 alkyl group, and R2 represents a C1-6 alkyl group, a C3-6 cycloalkyl group, a (C3-6 cycloalkyl)(C1-6 alkyl) group, a C6-10 aryl group, or a C7-12 aralkyl group).
摘要:
A novel method for preparing 5-[2-(methylthio)ethoxy]pyrimidin-2-amine useful as a regent or raw material for manufacture of medicaments, agricultural chemicals, and industrial products, which comprises alkanoylating the amino group of a 2-amino-4-alkoxypyrimidine, then converting the resultant into a 4-hydroxypyrimidine compound by a treatment with anhydrous aluminum chloride, further etherifying the 4-hydroxypyrimidine compound by a reaction with a 2-haloethyl methyl sulfide in the presence of a base, and removing the alkanoyl group to obtain 5-[2-(methylthio)ethoxy]pyrimidin-2-amine.