Electric Literature of 1450754-38-7, A common heterocyclic compound, 1450754-38-7, name is 3-(But-3-yn-1-yl)-3-(2-iodoethyl)-3H-diazirine, molecular formula is C7H9IN2, 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 mixture of 3-(but-3-yn-1-yl)-3-(2-iodoethyl)-3H-diazirine (70 mg, 282 imol, 1 eq) and 4- hydroxybenzaldehyde (34.5 mg, 282 imol, 1 eq) in 1 mL of DMF was added Cs2CO3 (276 mg, 847 imol, 3 eq) in one portion at 15C under N2. The mixture was stirred at 60 C for 12 hours.The residue was poured into 2 mL water. The aqueous phase was extracted with three 1 mL portions of ethyl acetate. The combined organic phases were washed twice with 2 mL of brine, dried with anhydrous Na2SO4, filtered and concentrated in vacuo to give 40 mg of crude aldehyde A-i as yellow oil which was used into the next step without further purification.
The synthetic route of 1450754-38-7 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; AQUINNAH PHARMACEUTICALS, INC.; BURNETT, Duane, A.; VACCA, Joseph, P.; (310 pag.)WO2018/119395; (2018); A1;,
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com