On January 7, 2010, Marsilje, Thomas H., III; Lu, Wenshuo; Chen, Bei; He, Xiaohui; Lee, Christian Cho-Hua; Jiang, Songchun; Yang, Kunyong published a patent.Synthetic Route of 152626-77-2 The title of the patent was Preparation of substituted 2-(phenylamino)pyrimidin-4-amine as IGF-1 receptor and anaplastic lymphoma kinase inhibitors for treating proliferative disorders. And the patent contained the following:
The invention is related to the preparation of pyrimidine derivatives I [ring E may optionally contain a double bond; one of Z1-3 = NR6, N(R6)(:O) or S(O)1-2 and the others are CR2; R6 = H, azetidin-3-yl, 1,1-dioxo-2H-thiopyran-4-yl,, (un)substituted alk(en/yn)yl, 4-(pyrrolidin-1-yl)-1-oxobutyl, 3-morpholinopropylsulfonyl, etc.; R2 = (un)substituted 2-oxo-1,2-dihydropyridin-3-yl, 2-oxoazepan-3-yl, 5-6 membered heteroaryl containing 1-3 heteroatoms selected from N, O and S; R1 = halo, optionally halogenated alkyl; R3, R4 = H; R5 = halo, OH, alkyl, alkoxy, CN, etc.; X = Y = (CH)0-1; m = 2-4] and their physiol. acceptable salts which may be used to treat, ameliorate or prevent a condition which responds to inhibition of insulin-like growth factor (IGF-1R) or anaplastic lymphoma kinase (ALK), and to their pharmaceutical compositions Thus, monoamination of 2,5-dichloro-N-(5-methyl-1H-pyrazol-3-yl)pyrimidin-4-amine (preparation given) with tert-Bu 4-(4-amino-5-fluoro-2-methylphenyl)piperidine-1-carboxylate (preparation given) and reductive amination of formaldehyde gave II. Selected I had IC50 values in the range of 1 nM – 1 μM for the inhibition of IGF-1R. The experimental process involved the reaction of 4-Bromo-5-methoxy-2-methylaniline(cas: 152626-77-2).Synthetic Route of 152626-77-2
The Article related to phenylaminopyrimidineamine preparation igf1r anaplastic lymphoma kinase inhibitor antiproliferative neoplasm, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Synthetic Route of 152626-77-2
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