On March 30, 2021, Guo, Hongli; Chen, Tao; Zhou, Feng; Gao, Daxin; Chen, Dawei published a patent.Reference of (R)-(4-Methylmorpholin-3-yl)methanol The title of the patent was Preparation of quinazoline-based compounds as KRAS G12C inhibitor for treatment and/or alleviation of KRAS G12C-related diseases. And the patent contained the following:
The present invention relates to preparation of quinazoline-based compounds as KRAS G12C inhibitor for treatment and/or alleviation of KRAS G12C-related diseases. In particular, the quinazoline-based compound I (wherein, α and β bonds are single bonds or double bonds, resp.; X = N or CR2; when the β bond is a single bond, Y = C(O) and Z = NR3; when the β bond is a double bond, Y and Z are independently N or CR2; when the α bond is a single bond, W = N and V = CH2 or C(O); when the a bond is a double bond, W = C and V = CR4 or N; U and M are each independently N, C or CH; ring A = Ph, 3-8 membered cycloalkyl, 5-6 membered heteroaryl or 4-8 membered heterocycloalkyl group; the A ring is unsubstituted or optionally substituted). Further, (ring B = 5-10 membered heterocycloalkyl; the B ring is unsubstituted or optionally substituted; R = C6-10 aryl, 5-10 membered heteroaryl or 9-14 membered fused heterocycloalkyl group; said R is unsubstituted or optionally substituted; R1 = C2-4 alkenyl, C2-4 alkynyl or partially unsaturated C4-6 cycloalkyl; said R1 is unsubstituted or optionally substituted; R2 = H, hydroxyl, halogen, cyano, amino etc.; R3 = C3-8 cycloalkyl, 3-8 membered heterocycloalkyl, C6-10 aryl, 5-10 heteroaryl, C3-8 cycloalkyl-C1-4 alkyl etc.; R4 = H, hydroxyl, halogen, C2-6 alkenyl, C2-6 alkynyl, cyano, amino etc.), its isomers, stable isotope derivatives or pharmaceutically acceptable salts were prepared The inventive compound and its composition disclosed can effectively treat diseases related to KRAS G12C, such as cancer. The experimental process involved the reaction of (R)-(4-Methylmorpholin-3-yl)methanol(cas: 1620510-51-1).Reference of (R)-(4-Methylmorpholin-3-yl)methanol
The Article related to quinazoline compound preparation kras g12c inhibitor antitumor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Reference of (R)-(4-Methylmorpholin-3-yl)methanol
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