Application of 1746-77-6, 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. 1746-77-6, name is Isopropyl carbamate belongs to amides-buliding-blocks compound, it is a common compound, a new synthetic route is introduced below.
To a mixture of 1-4 (120 mg, 294 imol, 1 eq), isopropyl carbamate (45.5 mg, 441 imol, 1.5eq) and Cs2CO3 (287.3 mg, 881 .9 imol, 3 eq) in dioxane (3 mL) was added XantPhos (34.0 mg,58.8 imol, 0.20 eq) and Pd2(dba)3 (26.9 mg, 29.4 imol, 0.10 eq) under an Argon atmosphere. The mixture was heated to 90C and stirred for 4 hours. The mixture was quenched by addition of 1 M HOAc and purified by prep-HPLC (column: Boston pH-lex 150*25 bum; mobile phase: [water(0.225%FormicAcid)-acetonitrile]; B%: 33%-63%,10 mm followedby further purification on column: Phenomenex Gemini C18 250*50mm*10 um; mobile phase:[water (0.05% ammonia hydroxide v/v)-acetonitrile]; B%: 28%-58%,12 mm). Compound 168was obtained as a yellow solid. 1H NMR (400 MHz, Methanol-d4), O ppm, 8.64 (br d, J = 2.26Hz, 1 H), 8.61 (br d, J = 2.64 Hz, 1 H), 8.44 (br s, 1 H), 8.10 (dd, J = 6.71, 2.70 Hz, 1 H), 7.60 -7.67 (m, 1 H), 7.33 (dd, J = 10.92, 9.16 Hz, 1 H), 5.25-5.47 (m, 1 H), 5.01 (dt, J = 12.52, 6.23Hz, 1 H), 4.32-4.43 (m, 2 H), 4.07-4.19 (m, 2 H), 1.33 (d, J = 6.27 Hz, 6 H). Method 1: RT =2.88 mm.; M+H = 431.1.
The synthetic route of Isopropyl carbamate has been constantly updated, and we look forward to future research findings.
Reference:
Patent; NOVARTIS AG; JIRICEK, Jan; LERARIO, Isabelle K.; LIANG, Fang; LIU, Xiaodong; MOLTENI, Valentina; NAGLE, Advait Suresh; NG, Shuyi Pearly; RATNIKOV, Maxim; SMITH, Jeffrey M.; XIE, Yongping; (167 pag.)WO2018/220531; (2018); A1;,
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