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医药中间体

医药中间体是指在药物合成过程中作为关键步骤的反应产物或原料物质,它们通常是化学结构较为简单的化合物,通过一系列化学反应可以转化为最终的药物成品。这些中间体在制药工业中扮演着重要角色,是实现复杂药物分子合成的关键组成部分。

特点
  1. 多样性:医药中间体种类繁多,根据所需药品的不同而不同。
  2. 复杂性:有些医药中间体本身可能较为简单,但通过一系列复杂的化学反应才能获得最终的药物成品。
  3. 安全性与纯度要求高:在制药行业中,医药中间体的安全性和纯度直接影响到最终产品的质量和效果。
应用
  1. 合成新药:许多复杂结构的新药都是通过一些简单的中间体经过一系列复杂的化学反应而合成得到的。
  2. 药物改良:通过对现有药物中的某些关键中间体进行优化,可以开发出更有效的治疗手段或者降低副作用。
  3. 原料供应保障:确保医药中间体的稳定供应对于维持药品市场供给至关重要。
生产与研发

医药中间体的研发和生产是一个复杂的过程,通常包括以下几个步骤:

  • 合成设计:根据目标药物结构设计合适的合成路线。
  • 实验室规模合成与优化:通过小规模实验来验证并优化反应条件。
  • 中试放大:将实验室中的成功方案应用于工业化生产前的中间试验阶段。
  • 工业化生产:在确保安全性和质量的前提下进行大规模生产。
发展趋势

随着化学合成技术的进步和新技术的应用(如绿色化学、计算机辅助设计等),医药中间体的研发与生产正朝着更加高效、环保的方向发展。同时,对药物分子结构的深入理解也为开发更有效的治疗方案提供了更多可能性。

中文名称 英文名称 CAS号 化学式 结构式图片
—— (R)-2-allyl-1-(7-ethyl-7-hydroxy-6,7-dihydro-5H-cyclopenta[b]pyridin-2-yl)-6-((4-(4-methylpiperazin-1-yl)phenyl)amino)-1,2-dihydro-3H-pyrazolo[3,4-d]pyrimidin-3-one 2376146-48-2 C29H34N8O2
(R)-2-allyl-1-(7-ethyl-7-hydroxy-6,7-dihydro-5H-cyclopenta[b]pyridin-2-yl)-6-((4-(4-methylpiperazin-1-yl)phenyl)amino)-1,2-dihydro-3H-pyrazolo[3,4-d]pyrimidin-3-one
—— 1,1'-bis[3-(trimethylammonium)propyl]-4,4'-bipyridinium tetrachloride 108228-37-1 C22H38N4*4Cl
1,1'-bis[3-(trimethylammonium)propyl]-4,4'-bipyridinium tetrachloride
—— 3-(tert-butylthio)-5-chloropyridine 123792-41-6 C9H12ClNS
3-(tert-butylthio)-5-chloropyridine
—— 3,5-Dibromo-2-chloro-6-(trifluoromethyl)pyridine 1845716-91-7 C6HBr2ClF3N
3,5-Dibromo-2-chloro-6-(trifluoromethyl)pyridine
—— 3-bromo-4-fluoro-2-methoxypyridine 1256810-67-9 C6H5BrFNO
3-bromo-4-fluoro-2-methoxypyridine
—— 4-aminocyclohexanesulfonic acid 146764-47-8 C6H13NO3S
4-aminocyclohexanesulfonic acid
—— (2R,3R,4R,5R,6R)-5-Acetamido-2-(acetoxymethyl)-6-(2-(2-(((benzyloxy)carbonyl)amino)ethoxy)ethoxy)tetrahydro-2H-pyran-3,4-diyl diacetate 1261568-35-7 C26H36N2O12
(2R,3R,4R,5R,6R)-5-Acetamido-2-(acetoxymethyl)-6-(2-(2-(((benzyloxy)carbonyl)amino)ethoxy)ethoxy)tetrahydro-2H-pyran-3,4-diyl diacetate
—— 22919-26-2 C10H9NaO6P
—— copper;1-hydroxypyridine-2-thione 154592-20-8 C5H5CuNOS
copper;1-hydroxypyridine-2-thione
—— 2,2'-Bicinchoninic acid dipotassium salt hydrate 63451-34-3 C20H12KN2O4
2,2'-Bicinchoninic acid dipotassium salt hydrate
—— (1R,8aS)-1-methyl-1-propan-2-yl-3,5,6,7,8,8a-hexahydro-[1,3]oxazolo[3,4-a]pyrazine 1321925-29-4 C10H20N2O
(1R,8aS)-1-methyl-1-propan-2-yl-3,5,6,7,8,8a-hexahydro-[1,3]oxazolo[3,4-a]pyrazine
—— 5-BROMO-2-THIENYLZINC BROMIDE 151073-94-8 C4H2Br2SZn
5-BROMO-2-THIENYLZINC BROMIDE
—— 3-Amino-6-methoxy-2-picoline hydrochloride 320577-63-7 C7H11ClN2O
3-Amino-6-methoxy-2-picoline hydrochloride
—— 1-O-methyl-2-deoxy-2-fluoro-3,5-O,O-dibenzyl-D-ribose 863642-44-8 C20H23FO4
1-O-methyl-2-deoxy-2-fluoro-3,5-O,O-dibenzyl-D-ribose
—— 3-(3-bromo-1H-pyrazol-1-yl)pyridine 1374320-72-5 C8H6BrN3
3-(3-bromo-1H-pyrazol-1-yl)pyridine
—— ethyl 3-chloro-5,6,7,8-tetrahydrocinnoline-4-carboxylate 32078-29-8 C11H13ClN2O2
ethyl 3-chloro-5,6,7,8-tetrahydrocinnoline-4-carboxylate
—— 1-hexyl-3-methylimidazolium dicyanamide 927902-57-6 C2N3*C10H19N2
1-hexyl-3-methylimidazolium dicyanamide
—— 6,7-dihydro-3-methyl-6-oxo-1-phenyl-1H-pyrazolo[3,4-b]pyridine-5-carbonitrile 52217-38-6 C14H10N4O
6,7-dihydro-3-methyl-6-oxo-1-phenyl-1H-pyrazolo[3,4-b]pyridine-5-carbonitrile
—— 2,6-bis[1-((2,6-diethylphenyl)imino)ethyl]pyridine 420119-94-4 C29H35N3
2,6-bis[1-((2,6-diethylphenyl)imino)ethyl]pyridine
—— 7α-Hydroxy-3-keto-Δ<sup>4</sup>-cholensaeure 14772-95-3 C24H36O4
7α-Hydroxy-3-keto-Δ<sup>4</sup>-cholensaeure
—— (R)-2-amino-3-(7-methyl-1Hindazol-5-yl)propanoic acid 1061710-38-0 C11H13N3O2
(R)-2-amino-3-(7-methyl-1Hindazol-5-yl)propanoic acid
—— Tucatinib hemiethanolate 1429755-56-5 C54H54N16O5
Tucatinib hemiethanolate
—— (1R,2R)-2-[(R)-3-(benzyloxy)pyrrolidin-1-yl]cyclohexanol 900513-88-4 C17H25NO2
(1R,2R)-2-[(R)-3-(benzyloxy)pyrrolidin-1-yl]cyclohexanol
—— tert-butyl (R)-2-((tert-butoxycarbonyl)amino)-3-iodopropanoate 1057341-65-7 C12H22INO4
tert-butyl (R)-2-((tert-butoxycarbonyl)amino)-3-iodopropanoate
—— 2-picoline N-oxide 931-19-1 C6H7NO
2-picoline N-oxide
—— (E)-tert-butyl 4-(2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)vinyl)piperidine-1-carboxylate 1160924-51-5 C18H32BNO4
(E)-tert-butyl 4-(2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)vinyl)piperidine-1-carboxylate
—— 17-Iodandrosta-5,16-dien-3β-ol 32138-69-5 C19H27IO
17-Iodandrosta-5,16-dien-3β-ol
—— 2,3-dichloro-4-iodofuro[2,3-c]pyridin-7-amine 1326713-71-6 C7H3Cl2IN2O
2,3-dichloro-4-iodofuro[2,3-c]pyridin-7-amine
—— Cis-4-Aminocyclohexanol 6850-65-3 C6H13NO
Cis-4-Aminocyclohexanol
—— 4727-41-7 C4H8O2S
—— 3,5-Dinitropyridin-2-olate 222548-10-9 C5H2N3O5-
3,5-Dinitropyridin-2-olate
—— 2-Methyl-2-propanyl (2S)-2-({[(2-methyl-2-propanyl)(diphenyl)silyl]oxy}methyl)-5-oxo-1-pyrrolidinecarboxylate 138871-56-4 C26H35NO4Si
2-Methyl-2-propanyl (2S)-2-({[(2-methyl-2-propanyl)(diphenyl)silyl]oxy}methyl)-5-oxo-1-pyrrolidinecarboxylate
—— methyl (penta-O-acetyl-3-deoxy-α-D-gluco-2-octulopyranosid)onate 66053-62-1 C19H26O13
methyl (penta-O-acetyl-3-deoxy-α-D-gluco-2-octulopyranosid)onate
—— 2,8-dibromo-[1,2,4]triazolo[1,5-a]pyridine 1257705-07-9 C6H3Br2N3
2,8-dibromo-[1,2,4]triazolo[1,5-a]pyridine
—— 2-amino-6-methyl-5,6,7,8-tetrahydro-1H-pteridin-4-one,dihydrochloride 69113-63-9 C7H10N4O*2ClH
2-amino-6-methyl-5,6,7,8-tetrahydro-1H-pteridin-4-one,dihydrochloride
—— 1-amino-4-cyclobutylpiperazine 61379-68-8 C8H17N3
1-amino-4-cyclobutylpiperazine
—— (1-ethyl-1,3,4,9-tetrahydro-pyrano[3,4-<i>b</i>]indol-1-yl)-acetic acid ethyl ester 111962-14-2 C17H21NO3
(1-ethyl-1,3,4,9-tetrahydro-pyrano[3,4-<i>b</i>]indol-1-yl)-acetic acid ethyl ester
—— 3-methyl-5-oxopyrrolidine-3-carboxylic acid 1508803-85-7 C6H9NO3
3-methyl-5-oxopyrrolidine-3-carboxylic acid
—— 6-Cbz-1-hydroxy-6-aza-spiro[3.4]octane 1419101-06-6 C15H19NO3
6-Cbz-1-hydroxy-6-aza-spiro[3.4]octane
—— 3,3-Oxetanediyldimethanamine dihydrochloride 111511-89-8 C5H12N2O*2ClH
3,3-Oxetanediyldimethanamine dihydrochloride
—— 3,4,6-tri-O-acetyl-2-deoxy-2-phthalimido-D-galactopyranose 72858-55-0 C20H21NO10
3,4,6-tri-O-acetyl-2-deoxy-2-phthalimido-D-galactopyranose
—— 2,5-DIMETHYLPYRAZOLO(1,5-A)PYRIMIDIN-7-ONE 98488-10-9 C8H9N3O
2,5-DIMETHYLPYRAZOLO(1,5-A)PYRIMIDIN-7-ONE
—— 2,3-Diaminobenzoate 603-81-6 C7H7N2O2-
2,3-Diaminobenzoate
—— (5-{5-(4-{[2-(4-chloro-phenyl)-4,4-dimethyl-cyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-[({3-nitro-4-[tetrahydro-2H-pyran-4-ylmethylamino]phenyl}sulfonyl)carbamoyl]phenoxy}-7H-pyrrolo[2,3-b]pyridin-7-yl)methyldihydrogenphosphate 1351456-78-4 C46H53ClN7O11PS
(5-{5-(4-{[2-(4-chloro-phenyl)-4,4-dimethyl-cyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-[({3-nitro-4-[tetrahydro-2H-pyran-4-ylmethylamino]phenyl}sulfonyl)carbamoyl]phenoxy}-7H-pyrrolo[2,3-b]pyridin-7-yl)methyldihydrogenphosphate
—— 4-Nitrophenyl-2,3,4,6-tetra-O-acetyl-β-D-glucopyranosid 2872-66-4 C20H23NO12
4-Nitrophenyl-2,3,4,6-tetra-O-acetyl-β-D-glucopyranosid
—— 3-(3-bromophenyl)-2-oxopropanoic acid 207910-90-5 C9H7BrO3
3-(3-bromophenyl)-2-oxopropanoic acid
—— Unii-3LM5SX2N4X 868171-91-9 C50H86O35P4
Unii-3LM5SX2N4X
—— tert-butyl 2-azabicyclo[3.1.0]hexane-2-carboxylate 154874-95-0 C10H17NO2
tert-butyl 2-azabicyclo[3.1.0]hexane-2-carboxylate
—— ((2S,5R)-5-aminotetrahydro-2H-pyran-2-yl)methanol 1398569-79-3 C6H13NO2
((2S,5R)-5-aminotetrahydro-2H-pyran-2-yl)methanol
—— 1-(3-methyl-2-pyridinyl)piperazine dihydrochloride 111960-11-3 C10H15N3*ClH
1-(3-methyl-2-pyridinyl)piperazine dihydrochloride