Unibest 优贝德
← 返回专利悬崖列表

CAS 73874-95-0

1,1-Dimethylethyl piperidin-4-ylcarbamate

登记编号:(IV)1055986-1-a,(IV)1055986-1-c、(VIII)1157260-1-a、(VI)1157260-2-a

应用背景(按来源药适应症)

肢端肥大症Paltusotine肠道肿瘤Paltusotine恶性类癌综合征Paltusotine腹泻Paltusotine肝癌Paltusotine回肠肿瘤Paltusotine非小细胞肺癌宗艾替尼肺癌宗艾替尼食道腺癌宗艾替尼食管胃结合部肿瘤宗艾替尼胃癌宗艾替尼转移性乳腺癌宗艾替尼

来源药(使用该中间体的合成路线)

品种梯队到期年
PaltusotineTier C · 观察 / 贸易-
宗艾替尼ZongertinibTier C · 观察 / 贸易-

合成路线中的位置(上下游链)

按路线登记顺序排列,左→右为合成方向;高亮为当前 CAS,其余可点击跳转对应档案。

Paltusotine优化路线步数:3总收率:/
6-Bromoquinolin-4-ol→6-Bromo-3-chloroquinolin-4-ol→4,6-Dibromo-3-chloroquinoline→1,1-Dimethylethyl piperidin-4-ylcarbamate→N-Boc-1-(6-bromo-3-chloroquinolin-4-yl)piperidin-4-amine→6-Bromo-4-chloroquinoline→N-Boc-1-(6-bromoquinolin-4-yl)piperidin-4-amine→2-Hydroxy-3-cyano-potassium phenyltrifluoro borate→(3-Cyano-2-hydroxyphenyl)boronic acid→N-Boc-3-[4-(4-aminopiperidin-1-yl)-3-chloroquinolin-6-yl]-2-hydroxybenzonitrile→(3,5-Difluorophenyl)Boranediol→N-Boc-1-(6-(3-cyano-2-hydroxyphenyl)-3-(3,5-difluorophenyl)quinolin-4-yl)piperidin-4-amine→3-[4-(4-Aminopiperidin-1-yl)-3-(3,5-difluorophenyl)quinolin-6-yl]-2-hydroxybenzonitrile dihydrogen chloride→3-[4-(4-Aminopiperidin-1-yl)-3-(3,5-difluorophenyl)quinolin-6-yl]-2-hydroxybenzonitrile→2-Bromo-6-cyanophenol→3-Bromo-2-(methoxymethoxy)benzonitrile
Paltusotine优化路线步数:5总收率:/
1,1-Dimethylethyl piperidin-4-ylcarbamate→N-Boc-1-(6-bromo-3-chloroquinolin-4-yl)piperidin-4-amine→(3,5-Difluorophenyl)Boranediol→3-[4-(4-Aminopiperidin-1-yl)-3-(3,5-difluorophenyl)quinolin-6-yl]-2-hydroxybenzonitrile→6-Bromo-3,4-dichloroquinoline→2-[(2-Methoxyethoxy)methoxy]-3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzonitrile→N-Boc-1-(3-chloro-6-[3-cyano-2-(2-methoxy-ethoxymethoxy)-phenyl]-quinolin-4-yl)-piperidin-4-amine→tert-Butyl [1-[3-chloro-6-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)quinolin-4-yl]piperidin-4-yl]carbamate→3-Bromo-2-[(2-methoxyethoxy)methoxy]benzonitrile→tert-Butyl [1-[6-[3-cyano-2-[(2-methoxyethoxy)methoxy]phenyl]-3-(3,5-difluorophenyl)quinolin-4-yl]piperidin-4-yl]carbamate
宗艾替尼优化路线步数:7总收率:/
1-Fluoro-2-methyl-4-nitrobenzene→1-Methyl-1H-1,3-benzimidazol-5-ol→1-Methyl-5-(2-methyl-4-nitrophenoxy)-1H-1,3-benzimidazole→3-Methyl-4-((1-methyl-1H-benzimidazol-5-yl)oxy)benzenamine→4-Chloro-6-(methylthio)pyrimido[5,4-d]pyrimidine→8-Chloro-2-(methylsulfanyl)pyrimido[5,4-d]pyrimidine hydrogen chloride→N-[3-Methyl-4-[(1-methyl-1H-1,3-benzimidazol-5-yl)oxy]phenyl]-6-(methylsulfanyl)pyrimido[5,4-d]pyrimidin-4-amine→6-(Methanesulfinyl)-N-[3-methyl-4-[(1-methyl-1H-1,3-benzimidazol-5-yl)oxy]phenyl]pyrimido[5,4-d]pyrimidin-4-amine→1,1-Dimethylethyl piperidin-4-ylcarbamate→tert-Butyl [1-(8-[3-methyl-4-[(1-methyl-1H-1,3-benzimidazol-5-yl)oxy]anilino]pyrimido[5,4-d]pyrimidin-2-yl)piperidin-4-yl]carbamate→6-(4-Aminopiperidin-1-yl)-N-[3-methyl-4-[(1-methyl-1H-1,3-benzimidazol-5-yl)oxy]phenyl]pyrimido[5,4-d]pyrimidin-4-amine→2-Propenoyl chloride
宗艾替尼优化路线步数:7总收率:/
6-(Methylsulfanyl)-[1,3]diazino[5,4-d]pyrimidin-4-ol→4-Chloro-6-(methylthio)pyrimido[5,4-d]pyrimidine→3-Methyl-4-((1-methyl-1H-benzimidazol-5-yl)oxy)benzenamine→N-[3-Methyl-4-[(1-methyl-1H-1,3-benzimidazol-5-yl)oxy]phenyl]-6-(methylsulfanyl)pyrimido[5,4-d]pyrimidin-4-amine→N-[3-Methyl-4-[(1-methyl-1H-1,3-benzimidazol-5-yl)oxy]phenyl]-6-(methylsulfanyl)pyrimido[5,4-d]pyrimidin-4-amine hydrogen chloride→6-(Methanesulfonyl)-N-[3-methyl-4-[(1-methyl-1H-1,3-benzimidazol-5-yl)oxy]phenyl]pyrimido[5,4-d]pyrimidin-4-amine→1,1-Dimethylethyl piperidin-4-ylcarbamate→tert-Butyl [1-(8-[3-methyl-4-[(1-methyl-1H-1,3-benzimidazol-5-yl)oxy]anilino]pyrimido[5,4-d]pyrimidin-2-yl)piperidin-4-yl]carbamate→6-(4-Aminopiperidin-1-yl)-N-[3-methyl-4-[(1-methyl-1H-1,3-benzimidazol-5-yl)oxy]phenyl]pyrimido[5,4-d]pyrimidin-4-amine hydrogen chloride (1/3)→(Chloromethyl)acetyl chloride→3-Chloro-N-[1-(8-[3-methyl-4-[(1-methyl-1H-1,3-benzimidazol-5-yl)oxy]anilino]pyrimido[5,4-d]pyrimidin-2-yl)piperidin-4-yl]propanamide

本站可供应的对应中间体

目录暂未收录该靶点的在售中间体 —— 可直接发起询价,需求会进入撮合池。

本页为中间体 CAS 注册档案:同 CAS 的多条路线登记已合并;后续供应商报价与买方需求以该 CAS 为主键撮合。