Abstract:
A beta-substituted Morita-Baylis-Hillman derivative, its preparation method, and its stereoisomer are provided to obtain a compound useful as an anticancer drug or an antiviral agent and useful for the treatment of the infectious disease caused by the bacteria which are parasitic within cells such as tuberculosis and leprosy. A beta-substituted Morita-Baylis-Hillman derivative is represented by the formula 1, wherein R_1a and R_1b are independently hydrogen, halo, hydroxy, alkyl, cycloalkyl, alkenyl, alkynyl, alkoxy or aryl group; X_1 is OR_4, or NR_(5a)R_(5b); X_2 is oxygen, sulfur or NR_6; R_2 is hydrogen, halo, hydroxy, alkyl, cycloalkyl, alkenyl, alkynyl, alkoxy or aryl; R_3a and R_3b are independently hydrogen, halo, hydroxy, alkyl, cycloalkyl, alkenyl, alkynyl, alkoxy or aryl; and methyl-2-(1-hydroxy-2-oxopropyl)hexadeca-2-noate is excluded in the compound of the formula 1.
Abstract translation:提供β-取代的Morita-Baylis-Hillman衍生物及其制备方法及其立体异构体以获得可用作抗癌药物或抗病毒剂的化合物,并且可用于治疗由寄生在其中的细菌引起的感染性疾病 细胞如结核病和麻风病。 β-取代的Morita-Baylis-Hillman衍生物由式1表示,其中R_1a和R_1b独立地为氢,卤素,羟基,烷基,环烷基,烯基,炔基,烷氧基或芳基; X_1为OR_4,或NR_(5a)R_(5b); X_2是氧,硫或NR_6; R 2是氢,卤素,羟基,烷基,环烷基,烯基,炔基,烷氧基或芳基; R_3a和R_3b独立地是氢,卤素,羟基,烷基,环烷基,烯基,炔基,烷氧基或芳基; 并且在式1的化合物中不包括甲基-2-(1-羟基-2-氧代丙基)十六烷-2-基。
Abstract:
A beta-substituted morita-baylis-hillman derivative is provided to be used as an anti-cancer agent or antiviral agent, and to treat infectious disease caused by bacteria which is parasitic on cells. A beta-substituted morita-baylis-hillman derivative has a structure represented by chemical formula 1. In chemical formula 1, R1a and R1b independently show hydrogen, hollow, hydroxy, alkyl, cycloalkyl, alkenyl, alkenyl, alkoxy or aryl, wherein one or more carbon atoms of alkyl, cycloalkyl, alkenyl, alkynyl or alkoxy can form a double bond with an oxygen atom; and X1 shows OR4 or NR5aR5b; X2 shows oxygen, sulfur or NR6.
Abstract:
The present invention relates to a chiral oxazaborolidinium ion catalyst and to an oxazaborolidinium ion which is used as a catalyst in a Roskamp reaction of making diazoester and aldehydes react to produce a chiral-beta-keto ester in the presence of a Lewis acid catalyst. The objective of the present invention is to provide a chiral-beta-keto ester compound which has high stereoselectivity at an alpha location.
Abstract:
An octahydro indeno derivative is provided to have a high biological activity, to have a high cytotoxin to cancer cells with a minimum amount and to be used as an anti-cancer drug or an antibiotic. A composition of treating and preventing cancers includes a compound indicated by a chemical formula 1 and a pharmaceutically allowed carrier. In the chemical formula 1: X is oxygen, sulfur or NH; R1 is hydrogen, hollow, hydroxy, alkyl, cycloalkyl, alkenyl, alkynyl or alkoxy; R2 and R3 are independently hydrogen, hollow, hydroxy, alkyl, cycloalkyl, alkenyl, alkynyl, alkoxy, aryl or heteroaryl; R4a and R4b are hydrogen, hollow, hydroxy, alkyl, cycloalkyl, alkenyl, alkynyl or alkoxy; R5a and R5b are hydrogen, hollow, hydroxy, alkyl, alkenyl, alkynyl or alkoxy; R6a and R6b are hydrogen, hollow, hydroxy, alkyl, alkenyl, alkynyl, alkoxy or the carbonyl radical; R7a and R7b are the hydrogen, hollow, hydroxy, alkyl, alkenyl, alkynyl or alkoxy; R8 is hydrogen, hollow, hydroxy, alkyl, alkenyl, alkynyl or alkoxy; and R9a and R9b are hydrogen, hollow, hydroxy, alkyl, cycloalkyl, alkenyl, alkynyl, alkoxy, aryl or heteroaryl.
Abstract:
PURPOSE: A method for enantioselectively synthesizing novel beta-substituted morita-baylis-hillman ester is provided to efficiently prepare products by enantioselective property for beta-substituted morita-baylis-hillman ester with optical activity. CONSTITUTION: A method for preparing a compound of below chemical formula 1 comprises the steps of: reacting a compound of chemical formula 2 with a compound of chemical formula 3 under the presence of a catalyst of chemical formula 4 and a solvent to prepare a compound of chemical formula 5; and substituting iodine of a compound of chemical formula 5 to prepare the compound of below chemical formula 1.