RESUMO
Here, we report O-methyl S-aryl thiocarbonates as a versatile esterification reagent for palladium-catalyzed methoxycarbonylation of arylboronic acid in the presence of copper(I) thiophene-2-carboxylate (CuTC). The reaction condition is mild, and a variety of substituents including sensitive -Cl, -Br, and free -NH2 could be tolerated. Further applications in the late-stage esterification of some pharmaceutical drugs demonstrate the broad utility of this method.
RESUMO
Palladium-catalyzed meta-selective C-H deuteration of a series of substrates, including phenylacetic acids, hydrocinnamic acid, benzylphosphonate, benzylsulfonate, and benzyl and phenyl ethyl alcohol ester, is developed by using a pyridine-based directing template. The template is installed into the substrate through a practical ester linkage. Under mild reaction conditions, a variety of phenylacetic acids containing alkyl, methoxyl, and halo substituents are compatible in the reaction, resulting in high levels of D-incorporation at the meta position.
RESUMO
OBJECTIVE: To explore the different effects of rectal application of Neiyi Kangfu Suppository (NYKFS) on the expressions of cytochrome C (Cyt C) and Survivin in ectopic and eutopic endometrium in endometriosis (EMT) model rats. METHODS: EMT rats were randomly divided into 6 groups, the high- and low-dose NYKFS groups, the Danazol Capsule (DN) group, the Dan'e Fukang Soft Extract (DFE) group, the model group and the blank group. The expressions of Cyt C and Survivin were measured using immunohistochemical SP staining method. RESULTS: (1) After treatment, the IOD value of Cyt C in ectopic endometrium significantly increased in the high-dose and low-dose NYKFS groups respectively to 6.08 +/- 0.35 and 6.23 +/- 0.35, which was significantly higher than that in the model group (5.07 +/- 0.70) and DFE group (5.98 +/- 1.02) respectively (P < 0.05, P < 0.01); while those of Survivin in ectopic endometrium was significantly decreased to 5.73 +/- 0.93 and 5.62 +/- 0.93 and was significantly lower than that in the model group (6.01 +/- 1.16, P < 0.05 or P < 0.01). (2) The lowered eutopic endometrial level of Cyt C in EMT rats after treatment was significantly higher in the two NYKFS groups than that in the model group (P < 0.05); while that of eutopic endometrial Survivin was insignificantly different between the NYKFS groups and the model group or the blank group (P > 0.05). CONCLUSION: NYKFS plays its role in inducing apoptosis by increasing the expression of Cyt C and decreasing the expression of Survivin in ectopic endometrium, but it up-regulates expression of Cyt C, has no obvious effect on Survivin expression in eutopic endometrium.