In the next few decades, the world population will flourish. As the population grows rapidly and people all over the world use more and more resources, all industries must consider their environmental impact. 2240-88-2, name is 3,3,3-Trifluoropropan-1-ol, the common compound, a new synthetic route is introduced below. COA of Formula: C3H5F3O
Tert-butyl [(lr,4r)-6′-bromo-4-methoxy-5″-methyl-3’H-dispiro[cyclohexane-l,2′-indene- ,2″- imidazol]-4″-yl]carbamate (Intermediate 12, 715 mg, 1.50 mmol), allylpalladium(II) chloride (21.95 mg, 0.06 mmol), di-tert-butyl(2′,4′,6′-triisopropyl-3-methoxy-6-methylbiphenyl-2- yl)phosphine (70.3 mg, 0.15 mmol) and CS2CO3 (733 mg, 2.25 mmol) were placed in a MW- vial. Toluene (8 mL) was added and the head space was evacuated and refilled with argon. 3,3,3- Trifluoropropan-l-ol (684 mg, 6.00 mmol) was added and the mixture was heated to 100 C in a MW apparatus for 2 h. 2 M methanolic ammonia (8.57 mL, 60.0 mmol) and water (1.08 mL, 60.0 mmol) was added and the mixture was heated to 80 C for 12 h. The reaction mixture was cooled to r.t. The organic solvents were evaporated and the aqueous residue was extracted with DCM. The combined extracts were concentrated and the residue was purified by reverse phase preparative chromatography providing the title compound (410 mg, 67% yield). 1H MR (500 MHz, DMSO-de) delta 0.90 (td, 1 H), 1.08 – 1.27 (m, 2 H), 1.34 – 1.49 (m, 3 H), 1.80 (d, 2 H), 2.15 (s, 3 H), 2.69 (tt, 2 H), 2.82 – 2.99 (m, 3 H), 3.15 – 3.22 (m, 3 H), 4.00 – 4.10 (m, 2 H), 6.08 (d, 1 H), 6.51 (br. s., 2 H), 6.75 (dd, 1 H), 7.18 (d, 1 H); MS (APCI+) m/z 410 [M+H]+.
The synthetic route of 2240-88-2 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; KARLSTROeM, Sofia; CSJERNYIK, Gabor; SWAHN, Britt-Marie; SANDBERG, Lars; KOLMODIN, Karin; SOeDERMAN, Peter; OeHBERG, Liselotte; WO2013/190298; (2013); A1;,
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