1231930-42-9

基本信息
LY2835219 中間體一
ABEMACICLIB 雜質(zhì)3
LY2835219中間體(KSM-1)
1-異丙基-2-甲基-4-氟-6-(2-氯-5-氟-4-嘧啶基)苯并咪唑
6-(2-氯-5-氟-4-嘧啶基)-4-氟-1-異丙基-2-甲基-1H-苯并咪唑
6-(2-氯-5-氟-嘧啶-4-基)-4-氟-1-異丙基-2-甲基-1H-苯并咪唑
6-(2-氯-5-氟嘧啶-4-基)-4-氟-1-異丙基-2-甲基-1H-苯并[D]咪唑
6-(2-氯-5-氟-4-嘧啶)-4-氟-2-甲基-1-(1-甲基乙基)-1H-苯并咪唑
6-(2-氯-5-氟-4-嘧啶基)-4-氟-2-甲基-1-(1-甲基乙基)-1H-苯并咪唑
LY2835219 intermediate
Abemaciclib intermediate
6-(2-chloro-5-fluoropyriMidin-4-yl)-4-fluoro
6-(2-Chloro-5-fluoro-4-pyrimidinyl)-4-fluoro-1-isopropyl-2-methylbenzimidazole
6-(2-chloro-5-fluoro-pyrimidin-4-yl)-4-fluoro-1-isopropyl-2-methyl-1H-benzoimidazole
6-(2-chloro-5-fluoropyriMidin-4-yl)-4-fluoro-1-isopropyl-2-Methyl-1H-benzo[d]iMidazole
1H-BenziMidazole, 6-(2-chloro-5-fluoro-4-pyriMidinyl)-4-fluoro-2-Methyl-1-(1-Methylethy
6-(2-chloro-5-fluoro-4-pyriMidinyl)-4-fluoro-2-Methyl-1-(1-Methylethyl)-1H-BenziMidazole
6-(2-chloro-5-fluoropyrimidin-4-yl)-4-fluoro-2-methyl-1-(propan-2-yl)-1H-1,3-benzodiazole
物理化學(xué)性質(zhì)
制備方法

1231930-37-2

2927-71-1

1231930-42-9
以4-氟-1-異丙基-2-甲基-6-硼酸頻哪醇酯基-1H-苯并[d]咪唑和2,4-二氯-5-氟嘧啶為原料,合成6-(2-氯-5-氟嘧啶-4-基)-4-氟-1-異丙基-2-甲基-1H-苯并咪唑的一般步驟如下:在氮?dú)獗Wo(hù)下,向4-氟-1-異丙基-2-甲基-6-(4,4,5,5-四甲基-1,3,2-二氧雜硼雜環(huán)戊烷-2-基)-1H-苯并[d]咪唑(318 mg,1 mmol)和2,4-二氯-5-氟嘧啶(166 mg,1 mmol)在6 mL乙腈中的懸浮液中,加入四(三苯基膦)鈀(115.6 mg,0.1 mmol)和2 mL飽和碳酸鈉水溶液。將反應(yīng)混合物加熱至85℃并攪拌8小時(shí)。反應(yīng)完成后,冷卻至室溫,用氯仿和異丙醇(體積比4:1)混合溶劑萃取。合并有機(jī)層,用飽和食鹽水洗滌,無水硫酸鈉干燥,過濾后減壓濃縮。粗產(chǎn)物通過硅膠柱色譜法純化,洗脫劑為二氯甲烷與甲醇的混合溶液(甲醇體積分?jǐn)?shù)0-10%),得到6-(2-氯-5-氟嘧啶-4-基)-4-氟-1-異丙基-2-甲基-1H-苯并咪唑(277 mg,產(chǎn)率86%)為灰色固體。LC-MS (m/z): 323.1 [M+H]+。
參考文獻(xiàn):
[1] Patent: WO2017/185031, 2017, A1. Location in patent: Page/Page column 96
[2] Tetrahedron Letters, 2015, vol. 56, # 7, p. 949 - 951
[3] Patent: US2010/160340, 2010, A1. Location in patent: Page/Page column 11
[4] Patent: WO2015/130540, 2015, A1. Location in patent: Page/Page column 22-23
[5] Patent: CN107266421, 2017, A. Location in patent: Paragraph 0043; 0052; 0053
報(bào)價(jià)日期 | 產(chǎn)品編號(hào) | 產(chǎn)品名稱 | CAS號(hào) | 包裝 | 價(jià)格 |
2025/05/22 | XW02123193042905 | 6-(2-氯-5-氟-嘧啶-4-基)-4-氟-1-異丙基-2-甲基-1H-苯并咪唑 | 1231930-42-9 | 10G | 342元 |
2025/05/22 | XW02123193042903 | 6-(2-氯-5-氟-嘧啶-4-基)-4-氟-1-異丙基-2-甲基-1H-苯并咪唑 | 1231930-42-9 | 1G | 39元 |
2025/05/22 | XW02123193042902 | 6-(2-氯-5-氟-嘧啶-4-基)-4-氟-1-異丙基-2-甲基-1H-苯并咪唑 | 1231930-42-9 | 250MG | 28元 |