达格列净合成工艺的改进
A new synthetic process of dapagliflozin
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摘要: 对SGLT2抑制剂达格列净的合成工艺进行改进。以1-氯-2-(4-乙氧基苄基)-4-碘苯和2,3,4,6-四乙酰氧基-α-D-溴代吡喃葡萄糖为原料,经格式交换,催化偶联以及乙酰基脱除反应,得到达格列净,总收率50%。本工艺反应步骤少,产生废料少,反应条件温和。Abstract: This paper describes a practical process for a SGLT2 inhibitor dapagliflozin. The target product was synthesized from 1-chloro-2-(4-ethoxybenzyl)-4-iodobenzene and 2, 3, 4, 6-tetra-O-acetyl-alpha-D-glucopyranosyl bromide by iodine-magnesium exchange, and coupling and acetyl removing reactions with the total yield of 50%. This practical process highlights fewer reaction steps, less waste and mild reaction conditions.
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Keywords:
- SGLT2 inhibitors /
- dapagliflozin /
- synthesis /
- process improvement /
- antidiabetic agents
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