63485-50-7, name is cis-Methyl 3-hydroxycyclobutanecarboxylate, belongs to esters-buliding-blocks compound, is considered to be a conventional heterocyclic compound, which is widely used in drug synthesis. The chemical synthesis route is as follows. Safety of cis-Methyl 3-hydroxycyclobutanecarboxylate
Triphenylphosphine (484 mg, 1 .85 mmol) was added to a solution of 2,5-difluorophenol (0.2 g, 1 .537 mmol) in tetrahydrofuran (1 .7 mL). The reaction mixture was cooled to 0 C, and (c/s)-methyl 3-hydroxycyclobutanecarboxylate (240 mg, 1 .85 mmol) was added, followed by DIAD (0.35 mL, 1 .8 mmol). After 10 min, the reaction mixture was warmed to room temperature, stirred for 3 days, and diluted with water and EtOAc. The mixture was partitioned, and the aqueous layer was extracted with EtOAc. The organic layer was washed with water, dried over sodium sulfate, filtered, and concentrated. The residue was purified on silica gel eluting with a 10%-60% EtOAc-heptane gradient to give the title compound (236 mg, 63%). 1H NMR (400 MHz, CDCI3) delta 2.48-2.59 (m, 2 H), 2.76 (ddd, J = 14, 7, 4 Hz, 2 H), 3.16-3.26 (m, 1 H), 3.75 (s, 3 H), 4.90 (quin, J = 7 Hz, 1 H), 6.49-6.63 (m, 2 H), 7.02 (ddd, J = 10, 9, 5 Hz, 1 H); LC-MS (LC-ES) M+H = 243.
The synthetic route of 63485-50-7 has been constantly updated, and we look forward to future research findings.
Reference:
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;,
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