Downstream synthetic route of 7405-23-4

The synthetic route of 7405-23-4 has been constantly updated, and we look forward to future research findings.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.7405-23-4,Benzo[d]thiazol-4-ol,as a common compound, the synthetic route is as follows.

Triphenylphosphine (9.72 g, 37.0 mmol) was added to a solution of benzo[d]thiazol-4- ol (4.00 g, 26.5 mmol) in tetrahydrofuran (80 ml_). The reaction mixture was cooled to 0 ¡ãC, and (c/s)-methyl 3-hydroxycyclobutanecarboxylate (4.13 g, 31 .7 mmol) was added, followed by the dropwise addition of DIAD (7.20 ml_, 37.0 mmol). The reaction mixture was then warmed to room temperature, stirred over the weekend, and concentrated. The remaining material was purified on silica gel eluting with a 15percent-60percent EtOAc-hexanes gradient. The appropriate fractions were combined, evaporated under reduced pressure and placed in vacuo to give the title compound (6.72 g, 90percent) which contained about 1 .1 equivalent of reduced DIAD contaminant. 1H NMR (400 MHz, CD3SOCD3) delta 2.51 -2.67 (m, 2 H), 2.75 (td, J = 7, 4 Hz, 2H), 3.10-3.19 (m, 1 H), 3.67 (s, 3 H), 5.03-5.10 (m, 1 H), 6.68 (d, J = 8 Hz, 1 H), 7.26 (t, J = 8 Hz, 1 H), 7.45 (d, J = 8 Hz, 1 H), 8.84 (s, 1 H); LC-MS (LC-ES) M+H = 264., 7405-23-4

The synthetic route of 7405-23-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED; DEATON, David Norman; GUO, Yu; HANCOCK, Ashley Paul; SCHULTE, Christie; SHEARER, Barry George; SMITH, Emilie Despagnet; STEWART, Eugene L.; THOMSON, Stephen Andrew; (556 pag.)WO2018/69863; (2018); A1;,
Thiazole | C3H3NS – PubChem
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