A novel and efficient method was developed for the liquid-phase synthesis of Nj,4-disubstitutedbenzodiazepine-2,5-diones with 2-chloro-5-nitrobenzoic acid as initiating material via 4 step reactions containing esterif...A novel and efficient method was developed for the liquid-phase synthesis of Nj,4-disubstitutedbenzodiazepine-2,5-diones with 2-chloro-5-nitrobenzoic acid as initiating material via 4 step reactions containing esterifieation, ＂Ulmn reaction＂, acylation, alkylation and cyclization. The reaction conditions were mild and the overall yields of the products ranged from 45% to 71%.展开更多
The copolymerization of DL-LA and 3-BMG was carried out in bulk with stannous 2-ethythexanoate as the catalyst. A series of copolymers with pendant protected groups were obtained and characterized by H-1-NMR and GPC a...The copolymerization of DL-LA and 3-BMG was carried out in bulk with stannous 2-ethythexanoate as the catalyst. A series of copolymers with pendant protected groups were obtained and characterized by H-1-NMR and GPC analysis. The monomer reactivity ratios were evaluated by the Fineman-Ross method and the Kelen-Tudos method and found to be r(BMG)=1.96 and r(LA)=0.37, respectively.展开更多
A simple and efficient protocol has been developed for the synthesis of 3-phenylnaphtho[2,3-b]furan-4,9-diones by domino reaction of a-bromonitroalkenes to 2-hydroxynaphthalene-1,4-dione. With the optimal reaction con...A simple and efficient protocol has been developed for the synthesis of 3-phenylnaphtho[2,3-b]furan-4,9-diones by domino reaction of a-bromonitroalkenes to 2-hydroxynaphthalene-1,4-dione. With the optimal reaction condi- tions [NaOAc （120 mol%）, water, 70 ~C, 7 h], the scope of the domino reaction was explored and the green ap- proach provided the desired products in moderate to good yields at elevated temperature under aqueous-mediated conditions. A mechanistic rationalization for this reaction is also provided. The absorption characteristics of the compounds were examined by UV-Vis spectra and fluorescence spectroscopy. All compounds were fluorescent in solution emitting at blue light （432--433 nm）, green light （512--536 nm）, or yellow light （591 nm）.展开更多
Steroidal drugs have wide indications such as anti-inflammation, anti-tumor, endocrine regulation,fertility management. Phytosterol is the main starting materials for the industrial synthesis of steroid drugs. Microbi...Steroidal drugs have wide indications such as anti-inflammation, anti-tumor, endocrine regulation,fertility management. Phytosterol is the main starting materials for the industrial synthesis of steroid drugs. Microbial transformation of phytosterol is a simple and environmentally friendly process. Efficient microbial strains for industrial phytosterol transformation are critical for the commercial success. To this end, a 96-well plate based method was developed to discriminate the mixture of 4-androstene-3,17-dione, androsta-1,4-diene-3,17-dione, and bisnoraldehyde, with different ratio of the 3 components in the mixture, which mimics the sterol bioconversion products by using the Mycobacterium neoaurum. The M. neoaurum bioconversed broth test using phytosterol as substrate also found that the spectrum methodology can evaluate the relative content of different compounds. The method is practical, high throughput and can replace the conventional HPLC-based assay for rapid selection of desired microbial strains.展开更多
基金Supported by the Natural Science Foundation of Hubei Province, China(No.2007ABA031)
文摘A novel and efficient method was developed for the liquid-phase synthesis of Nj,4-disubstitutedbenzodiazepine-2,5-diones with 2-chloro-5-nitrobenzoic acid as initiating material via 4 step reactions containing esterifieation, ＂Ulmn reaction＂, acylation, alkylation and cyclization. The reaction conditions were mild and the overall yields of the products ranged from 45% to 71%.
基金This work was supported by the Major State Basic Research Program of China (Grant No. G1999064704).
文摘The copolymerization of DL-LA and 3-BMG was carried out in bulk with stannous 2-ethythexanoate as the catalyst. A series of copolymers with pendant protected groups were obtained and characterized by H-1-NMR and GPC analysis. The monomer reactivity ratios were evaluated by the Fineman-Ross method and the Kelen-Tudos method and found to be r(BMG)=1.96 and r(LA)=0.37, respectively.
文摘A simple and efficient protocol has been developed for the synthesis of 3-phenylnaphtho[2,3-b]furan-4,9-diones by domino reaction of a-bromonitroalkenes to 2-hydroxynaphthalene-1,4-dione. With the optimal reaction condi- tions [NaOAc （120 mol%）, water, 70 ~C, 7 h], the scope of the domino reaction was explored and the green ap- proach provided the desired products in moderate to good yields at elevated temperature under aqueous-mediated conditions. A mechanistic rationalization for this reaction is also provided. The absorption characteristics of the compounds were examined by UV-Vis spectra and fluorescence spectroscopy. All compounds were fluorescent in solution emitting at blue light （432--433 nm）, green light （512--536 nm）, or yellow light （591 nm）.
文摘Steroidal drugs have wide indications such as anti-inflammation, anti-tumor, endocrine regulation,fertility management. Phytosterol is the main starting materials for the industrial synthesis of steroid drugs. Microbial transformation of phytosterol is a simple and environmentally friendly process. Efficient microbial strains for industrial phytosterol transformation are critical for the commercial success. To this end, a 96-well plate based method was developed to discriminate the mixture of 4-androstene-3,17-dione, androsta-1,4-diene-3,17-dione, and bisnoraldehyde, with different ratio of the 3 components in the mixture, which mimics the sterol bioconversion products by using the Mycobacterium neoaurum. The M. neoaurum bioconversed broth test using phytosterol as substrate also found that the spectrum methodology can evaluate the relative content of different compounds. The method is practical, high throughput and can replace the conventional HPLC-based assay for rapid selection of desired microbial strains.
