CAS 870-46-2

(tert-Butoxycarbonyl)hydrazinetert-butyl hydrazinecarboxylate

登记编号：(III)461018-9-a、ATAZ-005、GAND-025

应用背景（按来源药适应症）

华氏巨球蛋白血症伊布替尼慢性淋巴细胞白血病伊布替尼套细胞淋巴瘤伊布替尼移植物抗宿主病伊布替尼HIV感染硫酸阿扎那韦/考比司他HIV感染硫酸阿扎那韦获得性免疫缺损综合征硫酸阿扎那韦结核分枝杆菌感染硫酸阿扎那韦一型糖尿病硫酸阿扎那韦血液肿瘤Gandotinib骨髓纤维化Gandotinib骨髓增生性疾病Gandotinib原发性血小板增多症Gandotinib真性红细胞增多症Gandotinib

来源药（使用该中间体的合成路线）

品种	梯队	到期年
伊布替尼Ibrutinib	Tier A · 立即攻坚	2027
硫酸阿扎那韦/考比司他Atazanavir Sulfate/Cobicistat	Tier C · 观察 / 贸易	-
硫酸阿扎那韦Atazanavir Sulfate	Tier B · 提前布局	-
Gandotinib	Tier 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。

伊布替尼优化路线步数：6总收率：/

Pyrimidine-4-carbonitrile→6-Chloropyrimidine-4-carbonitrile→(tert-Butoxycarbonyl)hydrazine→6-Hydrazinylpyrimidine-4-carbonitrile hydrogen chloride→(Chloromethyl)acetyl chloride→3-Bromopropanoyl chloride→3-Bromopropanoyl bromide→4-Phenoxybenzaldehyde→3-(4-Phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine→N-Boc-3(S)-chloropiperidine→(R)-3-(4-phenoxyphenyl)-1-(piperidin-3-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine→1-[(3R)-3-[4-Amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]piperidin-1-yl]-3-chloropropan-1-one→1-[(3R)-3-[4-Amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]piperidin-1-yl]-3-bromopropan-1-one

硫酸阿扎那韦/考比司他原研路线步数：8总收率：/

4-bromobenzaldehyde→1-bromo-4-(dimethoxymethyl)benzene→2-bromopyridine→4-(pyridin-2-yl)benzaldehyde→tert-butyl hydrazinecarboxylate→tert-butyl (E)-2-(4-(pyridin-2-yl)benzylidene)hydrazine-1-carboxylate→tert-butyl 2-(4-(pyridin-2-yl)benzyl)hydrazine-1-carboxylate→tert-butyl ((S)-1-((R)-oxiran-2-yl)-2-phenylethyl)carbamate→tert-butyl 2-((2S,3S)-3-((tert-butoxycarbonyl)amino)-2-hydroxy-4-phenylbutyl)-2-(4-(pyridin-2-yl)benzyl)hydrazine-1-carboxylate→(2S,3S)-3-amino-4-phenyl-1-(1-(4-(pyridin-2-yl)benzyl)hydrazinyl)butan-2-ol→(S)-2-((methoxycarbonyl)amino)-3,3-dimethylbutanoic acid

硫酸阿扎那韦/考比司他工艺路线步数：7总收率：3.49 kg

2-bromopyridine→4-(pyridin-2-yl)benzaldehyde→tert-butyl hydrazinecarboxylate→tert-butyl (E)-2-(4-(pyridin-2-yl)benzylidene)hydrazine-1-carboxylate→tert-butyl 2-(4-(pyridin-2-yl)benzyl)hydrazine-1-carboxylate→tert-butyl ((S)-1-((R)-oxiran-2-yl)-2-phenylethyl)carbamate→tert-butyl 2-((2S,3S)-3-((tert-butoxycarbonyl)amino)-2-hydroxy-4-phenylbutyl)-2-(4-(pyridin-2-yl)benzyl)hydrazine-1-carboxylate→(2S,3S)-3-amino-4-phenyl-1-(1-(4-(pyridin-2-yl)benzyl)hydrazinyl)butan-2-ol→(S)-2-((methoxycarbonyl)amino)-3,3-dimethylbutanoic acid→(4-formylphenyl)boronic acid→tert-butyl ((2S,3R)-3,4-dihydroxy-1-phenylbutan-2-yl)carbamate→(6R,7S)-7-benzyl-2,2,3,3,11,11-hexamethyl-9-oxo-4,10-dioxa-8-aza-3-siladodecan-6-yl methanesulfonate→(2R,3S)-3-((tert-butoxycarbonyl)amino)-1-hydroxy-4-phenylbutan-2-yl methanesulfonate

硫酸阿扎那韦/考比司他优化路线步数：8总收率：/

tert-butyl hydrazinecarboxylate→tert-butyl 2-((2S,3S)-3-((tert-butoxycarbonyl)amino)-2-hydroxy-4-phenylbutyl)-2-(4-(pyridin-2-yl)benzyl)hydrazine-1-carboxylate→methyl 4-cyanobenzoate→methyl 4-(pyridin-2-yl)benzoate→4-(pyridin-2-yl)benzoic acid→(isobutyl carbonic) 4-(pyridin-2-yl)benzoic anhydride→(S)-tert-butyl (1-oxo-3-phenylpropan-2-yl)carbamate→(1R,2S)-2-((tert-butoxycarbonyl)amino)-1-cyano-3-phenylpropyl 4-(pyridin-2-yl)benzoate→tert-butyl (E)-2-((2R,3S)-3-((tert-butoxycarbonyl)amino)-4-phenyl-2-((4-(pyridin-2-yl)benzoyl)oxy)butylidene)hydrazine-1-carboxylate→tert-butyl 2-((2S,3S)-3-((tert-butoxycarbonyl)amino)-4-phenyl-2-((4-(pyridin-2-yl)benzoyl)oxy)butyl)hydrazine-1-carboxylate→tert-butyl 2-((2S,3S)-3-((tert-butoxycarbonyl)amino)-2-hydroxy-4-phenylbutyl)-2-(4-(pyridin-2-yl)benzoyl)hydrazine-1-carboxylate

硫酸阿扎那韦原研路线步数：8总收率：/

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