Brief introduction of 4175-72-8

The synthetic route of 4175-72-8 has been constantly updated, and we look forward to future research findings.

4175-72-8,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.4175-72-8,4-Chlorothiazole,as a common compound, the synthetic route is as follows.

[00262] To a thoroughly degassed solution of tert-butyl 4-(5,6-dichloro-2-iodo- pyrimidin-4-yl)-6,6-difluoro-1 ,4-diazepane-1 -carboxylate (3-003, prepared in scheme 3) (1 .6 g, 3.14 mmol), 4-chlorothiazole (0.38 g, 3.14 mmol) and cesium carbonate (1 .54 g, 4.71 mmol) in isoamyl alcohol (16 mL) was added palladium acetate (0.04 g, 0.157 mmol) and tri-tert- butylphosphonium tetrafluoroborate (0.09 g, 0.314 mmol). The mixture was heated to 90 C for 18 h. The reaction mixture was cooled before being diluted with ethyl acetate and 2 M HCI, and the two phases were separated. The aqueous was further extracted with ethyl acetate, the combined organics were dried (MgS04) and concentrated to dryness affording a dark brown film. The film was purified using flash chromatography on silica gel eluting with a mixture of ethyl acetate in cyclohexanes (0-50%). The desired fractions were concentrated to dryness to give the title compound (282 mg, 18%) as a brown film. LCMS: RT 5.82 min, Ml 502, Method (4LCMS1 ); NMR (400 MHz, CDCI3) delta 8.78 (s, 1 H), 4.49 (t, J = 12.1 Hz, 2H), 3.94 (s, 4H), 3.86 – 3.77 (m, 2H), 1 .49 (s, 9H).

The synthetic route of 4175-72-8 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; CANCER RESEARCH TECHNOLOGY LIMITED; CARSWELL, Emma L.; CHARLES, Mark David; EKWURU, Chukuemeka Tennyson; ELUSTONDO, Fred; FOWLER, Catherine M.; OTT, Gregory R.; ROFFEY, Jonathan R; BROOKFIELD, Joanna L.; FORD, Daniel; CALDER, Mathew L.; (159 pag.)WO2018/87527; (2018); A1;,
Thiazole | C3H3NS – PubChem
Thiazole | chemical compound | Britannica