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【结 构 式】

【分子编号】60243

【品名】N-{2-[(5-cyano-2-pyridinyl)amino]ethyl}guanidine

【CA登记号】

【 分 子 式 】C9H12N6

【 分 子 量 】204.23472

【元素组成】C 52.93% H 5.92% N 41.15%

与该中间体有关的原料药合成路线共 1 条

合成路线1

该中间体在本合成路线中的序号:(IX)

Condensation of 2-chloro-5-cyanopyridine (V) with ethylenediamine (VI) yields the N-pyridyl ethylenediamine (VII). Subsequent reaction of amine (VII) with pyrazole-1-carboxyamidine (VIII) in refluxing acetonitrile affords guanidine (IX). Finally, condensation between guanidine (IX) and enaminone (IV) in the presence of NaOEt produces the title pyrimidine derivative

1 Brown, S.P.; Goff, D.; Ring, D.B.; Harrison, S.D.; Subramanian, S.; Nuss, J.M.; Boyce, R.S.; Johnson, K.; Pfister, K.B.; Ramurthy, S.; Renhowe, P.A.; Seely, L.; Wagman, A.S.; Zhou, X.A. (Chiron Corp.); Inhibitors of glycogen synthase kinase 3. EP 1087963; US 6417185; WO 9965897 .
2 Ring, D.B.; Harrison, S.D.; Nuss, J.M.; Boyce, R.S.; Johnson, K.; Pfister, K.B.; Ramurthy, S.; Seely, L.; Wagman, A.S.; Desai, M.; Levine, B.H. (Chiron Corp.); Inhibitors of glycogen synthase kinase 3. WO 0220495 .
中间体序号 中间体编号 品名 CAS号 分子式 供应商 用于合成
(IV) 60242 1-(2,4-dichlorophenyl)-3-(dimethylamino)-2-(4-methyl-1H-imidazol-2-yl)-2-propen-1-one C15H15Cl2N3O 详情 详情
(V) 57164 2-Chloro-5-cyanopyridine; 6-Chloro-3-cyanopyridine; 6-Chloronicotinonitrile 33252-28-7 C6H3ClN2 详情 详情
(VI) 14754 ethylenediamine;1,2-Diaminoethane;ethane-1,2-diamine;1,2-Ethanediamine 107-15-3 C2H8N2 详情 详情
(VII) 54332 6-[(2-aminoethyl)amino]nicotinonitrile n/a C8H10N4 详情 详情
(VIII) 15983 1H-pyrazole-1-carboximidamide 4023-00-1 C4H6N4 详情 详情
(IX) 60243 N-{2-[(5-cyano-2-pyridinyl)amino]ethyl}guanidine C9H12N6 详情 详情
Extended Information