Abstract:
본 발명은 아토르바스타틴(상품명:리피토)을 제조하기 위한 핵심 중간체인, 4-(4-플루오르페닐)-2-이소부티릴-3-페닐-4-옥소- N -페닐-부티르아미드의 효율적인 제조방법에 관한 것으로서, 4-메틸-3-옥소- N -페닐펜타미드와 2-할로-1-(4-플루오르페닐)-2-페논 또는 2,2-디할로-1-(4-플루오르페닐)-2-페논을 염기 존재 하에서 친핵성 치환반응시키는 본 발명에 따르면 온화한 조건에서 높은 수율로 아트로바스타틴 제조용 중간체를 수득할 수 있다.
Abstract:
PURPOSE: A method for preparing bifenthrin is provided, to obtain bifenthrin with the improved production yield under the milder condition by employing the thioacyl dithiophosphate as an intermediate. CONSTITUTION: The method comprises the steps of reacting the 3-(2-chloro-3,3,3-trifluoro-1-propenyl)-2,2-dimethyl cyclopentane carboxylic acid alkyl ester represented by the formula 2 with the dithiophosphate represented by the formula 3 to prepare the thioacyl dithiophosphate represented by the formula 4; and reacting the thioacyl dithiophosphate of the formula 4 with the 2-methyl-biphenyl-3-yl-methanol represented by the formula 5 to prepare the bifenthrin represented by the formula 1, wherein R1 and R2 are an alkyl group of C1-C6, respectively. Preferably the first step is carried out with stirring the mixture in the presence of an amine base; and the second step is carried out in the presence of an amine base at a room temperature.
Abstract:
PURPOSE: Provided is a porphyrin derivative of the formula(1) which is useful as a photosensitizer in photodynamic therapy(PDT) applied to incurable diseases, such as cancer and the like. CONSTITUTION: The porphyrin derivative is represented by the formula(1), wherein R1, R2, R3, R4, R5, R6, R7 and R8 are identical or different each other, and represent hydrogen, an alkyl group or a heteroalkyl group containing a hetero atom; A1, A2, A3 and A4 are identical or different each other, and represent hydrogen, an alkyl group, a heteroalkyl group containing a hetero atom, an alkenyl group, a substituted or unsubstituted aryl group(wherein, a substituent is selected from a hydroxy group and a C1-C6 alkyl group) or a heteroaryl group; the alkyl group and alkenyl group represent a C1-C6 linear or branched hydrocarbon cycle; and the porphyrin derivative can be metalloporphyrin binding to a transition metal containing nickel.
Abstract:
PURPOSE: A method for preparing bifenthrin is provided, to obtain bifenthrin with the improved production yield under the milder condition by employing the thioacyl dithiophosphate as an intermediate. CONSTITUTION: The method comprises the steps of reacting the 3-(2-chloro-3,3,3-trifluoro-1-propenyl)-2,2-dimethyl cyclopentane carboxylic acid alkyl ester represented by the formula 2 with the dithiophosphate represented by the formula 3 to prepare the thioacyl dithiophosphate represented by the formula 4; and reacting the thioacyl dithiophosphate of the formula 4 with the 2-methyl-biphenyl-3-yl-methanol represented by the formula 5 to prepare the bifenthrin represented by the formula 1, wherein R1 and R2 are an alkyl group of C1-C6, respectively. Preferably the first step is carried out with stirring the mixture in the presence of an amine base; and the second step is carried out in the presence of an amine base at a room temperature.
Abstract:
Cephem derivs. of formula (I) are prepd. by (a) protecting amino gp. of 7-aminocephalosporanilic acid, (b) protecting carboxylic gp. on 4- position with methyl halide or diazomethane, (c) removing amino- protective gp., and (d) hydrolyzing with PLE (pig liver esterase) in an acetone aq. soln. In (I), R=H, (un)substd. alkyl, halogen, (un) substd. alkenyl or aromatic hetero gp.