Abstract:
PURPOSE: A process for preparing 4-hydroxy-N-benzyl-2-piperidinone is provided, thereby easily preparing 4-hydroxy-N-benzyl-2-piperidinone which is an intermediate for preparing atorvastatin useful as a hyperlipidemia treating agent with high yield under mild condition. CONSTITUTION: The process for preparing 4-hydroxy-N-benzyl-2-piperidinone represented by formula (2) comprises hydrogenating 2,4-dioxo-N-benzyl-piperidine of formula (3) in organic solvent in the presence of ruthenium catalyst at 100 deg. C and 30 to 100 atmosphere, wherein the organic solvent is selected from methanol, ethanol, isopropanol, t-butanol, methylene chloride, tetrahydrofuran, acetonitrile, t-butanol, dimethylformamide, diethylether, ethylacetate, acetone and chloroform; and the ruthenium catalyst is selected from Ru2Cl4(BINAP)2NEt3, Ru2Cl4(Tol-BINAP)2NEt3, Ru2Cl2(BINAP)2, Ru2Br2(MINAP)2, RuHCl(BINAP), Ru(BINAP)CO2(CH3)2 and Ru(Tol-BINAP)CO2(CH3)2 in which Tol is toluene, BINAP is 2,2'-bis(diphenylphosphino)-1,1'-binaphtyl.
Abstract:
본 발명은 하기 일반식(I)의 페넴 유도체 및 그의 약제학적으로 허용되는 염, 제조방법 및 이를 활성 성분으로 함유하는 항생제 조성물에 관한 것으로, 일반식(I)의 화합물은 경구흡수도가 높고, 항균력이 우수하여 항생제로 유용하다: (I) 상기식에서, R 1 은 수소, 카르복실기, 알릴, 카르복실 보호기 또는 약제학적으로 허용가능한 무기 또는 유기염이고; R 2 는 C 1- C 6 의 알킬기, C 3 -C 6 사이클릭 알킬기, C 3- C 10 의 방향족 알킬기 또는 C 2 -C 6 의 알케닐기이고; R 3 는 C 1- C 6 의 알킬기, C 3 -C 6 사이클릭 알킬기, 카바모일기 또는 아세틸기이다.
Abstract:
The invention provides 3-azabicyclo[3.1.3 heptane derivatives which are useful for preparation of novel quinolone and beta-lactam antibiotics and a process for producing said derivatives. These derivatives are represented by the formula (I) wherein; n is 0 or 1; each R1, R2 and R3 is hydrogen, low alkyly or amino protecting group such as benzyl and low alcoxycarbonyl; R4 is hydrogen, unsubstituted low alkyl group, or low alkyl group substituted by hydroxy, amino group, low alcoxy group, low alkylamino group or halogen.