Researchers who often do experiments know that organic synthesis is a process of preparing more complex target molecules from simple raw materials through one or more chemical reactions. Generally, it requires fewer steps, and cheap raw materials. 127946-77-4, name is 1-Amino-1-cyclopropanecarbonitrile hydrochloride, A new synthetic method of this compound is introduced below., category: nitriles-buliding-blocks
(3R,4R)-N-( 1 -Cyanocyclopropyl)-4-(5 -(4-( 1,1 -dioxidothiomorpholino)phenyl)-2-(5 – fluoropyridin-3 -yl)thiazol-4-yl)bicyclo [4.1 . 0]heptane-3 -carboxamide was synthesized following the same procedure as in Step H of Example 1 using (3R,4R)-4-(5-(4-(1,1- dioxidothiomorpholino)phenyl)-2-(5 -fluoropyridin-3 -yl)thiazol-4-yl)bicyclo [4.1 . 0]heptane-3 -carboxylic acid (0.180 g, 0.340 mmol, 1.00 equiv), DMF (5 mL), 1- aminocyclopropanecarbonitrile hydrochloride (0.202 g, 1.70 mmol, 5.00 equiv), HATU (0.324 g, 0.850 mmol, 2.50 equiv) and DIPEA (0.330 g, 2.55 mmol, 7.48 equiv). This resulted in 0.135 g (67%) of (3R,4R)-N-( 1 -Cyanocyclopropyl)-4-(5 -(4-( 1,1 -dioxidothiomorpholino)phenyl)-2-(5 – fluoropyridin-3-yl)thiazol-4-yl)bicyclo[4. 1 .0]heptane-3-carboxamide as a yellow solid: MS (ES,m/z): 592.1 (M + 1).
The basis of chemical reaction formula synthesis, the synthesis route is composed of some specific reactions and combined according to certain logical thinking. We look forward to the emergence of more reaction modes in the future.
Reference:
Patent; MERCK SHARP & DOHME CORP.; STACHEL, Shawn; PAONE, Daniel, V.; LI, Jing; GINNETTI, Anthony; LIM, John; FU, Jianmin; XU, Shimin; WO2015/54038; (2015); A1;,
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