On March 24, 2016, Shia, Kak-Shan; Jan, Jiing-Jyh; Tsou, Lun Kelvin; Chen, Chiung-Tong; Chao, Yu-Sheng published a patent.Safety of 2-(Oxiran-2-ylmethyl)isoindoline-1,3-dione The title of the patent was Preparation of quinazoline heterocyclic compounds and use thereof to mobilize hematopoietic stem cells and endothelial progenitor cells. And the patent contained the following:
Heterocyclic compounds I [wherein: M = (CH2)m; each of R1 and R2, independently, is H, halogen, NO2, CN, NH2, C1-6-alkyl, C1-6-alkoxy, C3-10-cycloalkyl, C1-10-heterocycloalkyl, aryl, or heteroaryl; or, R1 and R2, together with the two carbon atoms to which they are bonded, are C5-10-cycloalkyl, C3-10-heterocycloalkyl, aryl, or heteroaryl, each of alkyl, alkoxy, cycloalkyl, heterocycloalkyl, aryl, and heteroaryl being optionally substituted;]. [Each of R3 and R4, independently, is NRbRc, Z1 or Z2; in which: each of Rb and Rc, independently, is H or C1-6-alkyl;R5 is H, C1-6-alkyl, C3-10-cycloalkyl, C1-10-heterocycloalkyl, arylalkyl, heteroaryl alkyl, aryl, or heteroaryl; each of alkyl, cycloalkyl, heterocycloalkyl, arylalkyl, heteroarylalkyl, aryl, and heteroaryl being optionally substituted;]. [R6 is H, C1-6-alkyl, C1-6-alkoxy, C3-10-cycloalkyl, C1-10-heterocycloalkyl, aryl, or heteroaryl;L1 is heteroaryl, C1-10-heterocycloalkyl, NH, or NRd; in which Rd is C(:O)(CH2)2CHNH2CO2Re; Re being H, C1-6-alkyl, C3-10-cycloalkyl, C3-10-heterocycloalkyl, aryl, or heteroaryl;R7 is H, C1-6-alkyl, C1-6-alkoxy, C3-10-cycloalkyl, C1-10-heterocycloalkyl, aryl, or heteroaryl; each of alkyl, alkoxyl, cycloalkyl,heterocycloalkyl, aryl, and heteroaryl being optionally substituted;]. [M is 1 – 6; n is 1 – 6; each of R8 and R9, independently, is H, C1-6-alkyl, C3-10-cycloalkyl, C1-10-heterocycloalkyl, aryl, or heteroaryl; each of alkyl, cycloalkyl, heterocycloalkyl, aryl, and heteroaryl being optionally substituted; L2 is C1-6-alkyl; or L2, together with R8 8or R9 and the nitrogen atom to which they are bonded, is C4-10-heterocycloalkyl or heteroaryl; and,]. [R10 is H, C1-6-alkyl, C1-6-alkoxy, C3-10-cycloalkyl, C1-10-heterocycloalkyl, aryl, heteroaryl, arylalkyl, heteroarylalkyl, ester, amide thioamide, or acyl; each of alkyl, alkoxyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, aryl alkyl, and heteroaryl alkyl being optionally substituted] are shown herein. Thus, quinazoline II was prepared from 2,4-dichloroquinazoline via amination with tert-Bu 4-aminopiperidine-1-carboxylate; amination with aminotriazle III; and debutoxycarbonylation. The synthesis of II is also desribed. Also disclosed are pharmaceutical compositions containing the heterocyclic compounds and methods of using the heterocyclic compounds to mobilize hematopoietic stem cells and endothelial progenitor cells into the peripheral circulation. Further provided are methods for treating tissue injury, cancer, inflammatory disease, and autoimmune disease with the heterocyclic compounds The experimental process involved the reaction of 2-(Oxiran-2-ylmethyl)isoindoline-1,3-dione(cas: 5455-98-1).Safety of 2-(Oxiran-2-ylmethyl)isoindoline-1,3-dione
The Article related to heterocyclic compound preparation pharmaceutical composition mobilizer hematopoietic stem cells, tissue injury treatment quinazoline pyrimidine compound, cancer treatment quinazoline pyrimidine compound, inflammatory disease treatment quinazoline pyrimidine compound, autoimmune disease treatment quinazoline pyrimidine compound and other aspects.Safety of 2-(Oxiran-2-ylmethyl)isoindoline-1,3-dione
Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics