Application of 103878-09-7 ,Some common heterocyclic compound, 103878-09-7, molecular formula is C8H9NO3, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc., below Introduce a new synthetic route.
To a slurry of (iS,25T)-l-iV-(6-fluoi -l,3-benzothiazoi-2-yl)cyclopentane-l,2-diamine hydrochloride (Intermediate 1; 100 mg, 0.35 mmol) in dry DCM (1.2 ml) was added 3- ethoxypyridine-2-carboxylic acid hydrochloride (Intermediate 5, 78 mg, 0,38 mmol), HATU (198 mg, 0.52 mmol) and triethyiamine (145 mu, 1.04 mmol). The reaction mixture was stirred at room temperature for 17 hours then partitioned between DCM and a saturated solution of sodium bicarbonate. The organics were filtered through a (0581) hydrophobic frit and concentrated in vacuo. The crude material was purified by reverse phase preparative HPLC (eluted with acetonitriie / water containing 0.1 % ammonia) to afford the title compound. (0582) 1H MR (400 MHz, DCM-cfc) delta ppm 1.43 – 1.55 (m, 3 H), 1.64 – 1.77 (m, 2 H), 1.86 – 1.98 (m, 2 H), 2.23 – 2.36 (m, 1 H), 2.45 – 2.60 (m, 1 H), 3.96 – 4.09 (m. 1 H), 4.10 – 4.23 (m, 2 H), 4.31 – 4.48 (m, 1 H), 6.94 – 7.07 (m, 1 H), 7.24 – 7.33 (m, 1 H), 7.35 – 7,46 (m, 3 H), 8.06 – 8.24 (m, 2 H) (0583) MS ES+: 401
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,103878-09-7, its application will become more common.
Reference:
Patent; TAKEDA CAMBRIDGE LIMITED; TAKEDA PHARMACEUTICAL COMPANY LIMITED; FIELDHOUSE, Charlotte; GLEN, Angela; FUJIMOTO, Tatsuhiko; ROBINSON, John Stephen; WO2015/124934; (2015); A1;,
Pyridine – Wikipedia,
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