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Title: | Phương pháp tổng hợp exemestan từ họp chất androsta-1,4-dien-3,17-dion |
Authors: | Cao, Đức Tuấn Trịnh, Thị Hải Bạch, Thị Như Quỳnh Nguyễn, Hồng Thu Bùi, Thị Thắm Trịnh, Hiền Trung Phạm, Văn Thức Nguyễn, Văn Hùng |
Keywords: | Exemestane Steroid Breast cancer Androsta-1,4-dien-3,17-dione |
Issue Date: | 2018 |
Series/Report no.: | Tạp chí Dược học;Số 510 .- Tr.35-38 |
Abstract: | As regarding exemestane (1) as a 3rd-generation aromatase inhibitor widely used for treatment of hormone dependent breast cancer in postmenopausal women, it was synthesized with a 3-step method from androsta-1,4-diene-3,17-dione (2). Firstly, compound 2 was converted to 1,3-dipyrrolidinoandrosta-3,5-dien-17-on (3) and the intermediate product 3 was used immediately in the second step to afford 6-(hydroxymethyl)androsta-1,4-dien-3,17-dion (A), the combined yield of fist two steps was 77 %. In the final step, exemestane was archived from compound 4 with 88.2 % yield. The synthesis achieved the overall yield of 67.9 %. The structures of exemestane and intermediate products were confirmed by MS and NMR. |
URI: | https://dspace.ctu.edu.vn/jspui/handle/123456789/54661 |
ISSN: | 0866-7861 |
Appears in Collections: | Dược học |
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