Lọc theo danh mục
  • Năm xuất bản
    Xem thêm
  • Lĩnh vực
liên kết website
Lượt truy cập
 Lượt truy cập :  14,874,230

61.37

Kỹ thuật hóa học

Đỗ Thị Kim Phượng; Đoàn Thị Mai Hương; Vũ Văn Nam; Trần Văn Hiệu; Trương Bích Ngân; Lê Công Vinh; Phạm Văn Cường; Nguyễn Văn Hùng; Võ Thanh Giang; Châu Văn Minh; Đoàn Thị Mai Hương(1)Trương Bích Ngân(2)Trương Bích Ngân(3)Phạm Văn Cường(4)Vũ Văn Nam(5)

Nghiên cứu quy trình tổng hợp Febrifugine Hydrochloride

Study on synthesis procedure of febrifugine hydrochloride

Hóa học

2014

4

452-457

0866-7144

Febrifugine Hydrochloride; Tổng hợp; Nghiên cứu; Phân lập; Wngsd ụng

Febrifugine, a quinazoline alkaloid, isolated from Dichroa febrifuga roots, shows powerful antimalarial activity against Plasmodium falciparum. Strong liver toxicity has precluded febrifugine as a potential clinical drug. However, the potent antimalarial activity of febrifugine has stimulated medicinal chemists to pursue compounds derived from febrifugine, which may be valuable leads for novel drugs. Total synthesis and structural modification of febrifugine have been made. Among the reported asymmetric approaches to febrifugine, one of the most straight forward approaches to construct the 2-substituted 3-hydroxy piperidine is the stereoselective reaction of 3-hydroxy-piperidine N-acyliminium ions with the nucleophiles. In this study, the authors synthesized febrifugine hydrochloride (13) from L-glutamic acid (1) base on the asymmetric BF3.Et20 catalyzed nucleophilic reactions. The precursor 12 was formed by open epoxy ring using triethylamine and then oxidation with Dess-Martin periodinane. Their structures were established by MS and NMR spectroscopies.

TTKHCNQG, CVv 14