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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
—— 1-hydroxy-3-nitro-1<i>H</i>-pyridin-4-one 31872-57-8 C5H4N2O4
1-hydroxy-3-nitro-1<i>H</i>-pyridin-4-one
—— 3β-acetoxy-5α-pregn-16-en-20-one 1169-20-6 C23H34O3
3β-acetoxy-5α-pregn-16-en-20-one
—— quinidine hydrochloride monohydrate 6151-40-2 C20H24N2O2*ClH*H2O
quinidine hydrochloride monohydrate
—— 4H,8H-benzo<1,2-c:4,5-c'>bis<1,2,5>thiadiazole-4,8-dione 91120-84-2 C6N4O2S2
4H,8H-benzo<1,2-c:4,5-c'>bis<1,2,5>thiadiazole-4,8-dione
—— 3a,6a-dimethyl-1,3,4,6-tetrahydropentalene-2,5-dione 21170-10-5 C10H14O2
3a,6a-dimethyl-1,3,4,6-tetrahydropentalene-2,5-dione
—— 5-phenyl-5H-dibenzophosphole-5-oxide 1031-13-6 C18H13OP
5-phenyl-5H-dibenzophosphole-5-oxide
—— 2,4-difluoro-N-methylbenzamide 948717-18-8 C8H7F2NO
2,4-difluoro-N-methylbenzamide
—— 2-(4-methylphenyl)quinoline 24667-94-5 C16H13N
2-(4-methylphenyl)quinoline
—— 1,5-di(2-thienyl)-1,4-pentadien-3-one 886-78-2 C13H10OS2
1,5-di(2-thienyl)-1,4-pentadien-3-one
—— 2-(4-cyclopropyl-benzyl)-4-(β-D-glucopyranos-1-yl)-benzonitrile 946525-65-1 C23H25NO5
2-(4-cyclopropyl-benzyl)-4-(β-D-glucopyranos-1-yl)-benzonitrile
—— 1,4-bis(tetrahydro-2H-pyran-2-yloxy)benzene 2139-44-8 C16H22O4
1,4-bis(tetrahydro-2H-pyran-2-yloxy)benzene
—— L-Cephalexin 34632-04-7 C16H17N3O4S
L-Cephalexin
—— trans-4-Aminocyclohexanol 27489-62-9 C6H13NO
trans-4-Aminocyclohexanol
—— (3R-cis)-3-acetyloxy-4-phenyl-2-azetidinone 133066-59-8 C11H11NO3
(3R-cis)-3-acetyloxy-4-phenyl-2-azetidinone
—— N-(isopentyl)-quinolinium iodide 54899-89-7 C14H18N*I
N-(isopentyl)-quinolinium iodide
—— trans-4-hydroperoxycyclophosphamide 39800-16-3 C7H15Cl2N2O4P
trans-4-hydroperoxycyclophosphamide
—— umbellulone 546-78-1 C10H14O
umbellulone
—— 6-fluoro-1,2,3,4-tetrahydrobenzo[4,5]thieno[2,3-c]pyridine 685086-10-6 C11H10FNS
6-fluoro-1,2,3,4-tetrahydrobenzo[4,5]thieno[2,3-c]pyridine
—— tert-butyl (4R,5R)-2,2-dimethyl-4-[4-[4-[(2-methylpropan-2-yl)oxycarbonylamino]phenyl]-3-oxobutyl]-5-phenyl-1,3-oxazolidine-3-carboxylate 1426235-02-0 C31H42N2O6
tert-butyl (4R,5R)-2,2-dimethyl-4-[4-[4-[(2-methylpropan-2-yl)oxycarbonylamino]phenyl]-3-oxobutyl]-5-phenyl-1,3-oxazolidine-3-carboxylate
—— 1-[2-(2-hydroxyethoxy)ethyl]piperazine hydrochloride 85293-16-9 C8H18N2O2*2ClH
1-[2-(2-hydroxyethoxy)ethyl]piperazine hydrochloride
—— N-Fmoc-(O-N-acetylgalactosaminyl)threonine tert-butyl ester 189561-75-9 C31H40N2O10
N-Fmoc-(O-N-acetylgalactosaminyl)threonine tert-butyl ester
—— trans-4-Methycyclohexyl isocyanate 32175-00-1 C8H13NO
trans-4-Methycyclohexyl isocyanate
—— 1-aminodibenzothiophene 29451-76-1 C12H9NS
1-aminodibenzothiophene
—— 1-oxy-pyrazine-2,6-diamine 41536-72-5 C4H6N4O
1-oxy-pyrazine-2,6-diamine
—— 4-methoxyphenyl 2-(acetylamino)-2-deoxy-β-D-glucopyranoside 38229-78-6 C15H21NO7
4-methoxyphenyl 2-(acetylamino)-2-deoxy-β-D-glucopyranoside
—— 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]-4-methylpiperazine 1293489-87-8 C19H24N2S
1-[2-(2,4-dimethylphenylsulfanyl)phenyl]-4-methylpiperazine
—— 1-benzyl-1,2,3,6-tetrahydropyridin-4-en-3-one 94923-25-8 C12H13NO
1-benzyl-1,2,3,6-tetrahydropyridin-4-en-3-one
—— (2R,3S)-3-(6-chloro-5-fluoropyrimidin-4-yl)-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1 yl)butan-2-ol 137234-75-4 C16H13ClF3N5O
(2R,3S)-3-(6-chloro-5-fluoropyrimidin-4-yl)-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1 yl)butan-2-ol
—— ethyl (1S,5R)-2-oxo-3-oxabicyclo[3.1.0]hexane-1-carboxylate 145032-58-2 C8H10O4
ethyl (1S,5R)-2-oxo-3-oxabicyclo[3.1.0]hexane-1-carboxylate
—— (23S)-3α,7α,23-trihydroxy-5β-cholan-24-oic acid 105880-09-9 C24H40O5
(23S)-3α,7α,23-trihydroxy-5β-cholan-24-oic acid
—— 4-bromo-N-hydroxybenzenecarboximidoyl chloride 29203-58-5 C7H5BrClNO
4-bromo-N-hydroxybenzenecarboximidoyl chloride
—— methyl (E)-3-formylcrotonate 40835-18-5 C6H8O3
methyl (E)-3-formylcrotonate
—— 2'-O-methoxyethyl-5'-O-dimethoxytrityl-5-methylcytidine 182496-00-0 C34H39N3O8
2'-O-methoxyethyl-5'-O-dimethoxytrityl-5-methylcytidine
—— methyl 5-isoquinolyloxyacetate 130292-81-8 C12H11NO3
methyl 5-isoquinolyloxyacetate
—— 8-chloro-3-iodoquinoline 847727-21-3 C9H5ClIN
8-chloro-3-iodoquinoline
—— 2-[5-fluoro-1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]-5-[(E)-phenyldiazenyl]pyrimidine-4,6-diamine 1350653-29-0 C23H17F2N9
2-[5-fluoro-1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]-5-[(E)-phenyldiazenyl]pyrimidine-4,6-diamine
—— ethyl 5-fluoro-1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridine-3-carboxylate 1361232-72-5 C16H13F2N3O2
ethyl 5-fluoro-1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridine-3-carboxylate
—— ethyl 3-(2,6-dichloro-5-fluoropyridin-3-yl)-3-oxopropanoate 96568-04-6 C10H8Cl2FNO3
ethyl 3-(2,6-dichloro-5-fluoropyridin-3-yl)-3-oxopropanoate
—— 5-(but-1-yn-1-yl)-1-(tetrahydro-2H-pyran-2-yl)-1H-indazole 1365889-00-4 C16H18N2O
5-(but-1-yn-1-yl)-1-(tetrahydro-2H-pyran-2-yl)-1H-indazole
—— 1-{[(1E,2E)-3-(5-nitrofuran-2-yl)prop-2-ene-1-ylidene]amino}imidazolidin-2,4-dione 1672-88-4 C10H8N4O5
1-{[(1E,2E)-3-(5-nitrofuran-2-yl)prop-2-ene-1-ylidene]amino}imidazolidin-2,4-dione
—— N-(4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-2-yl)pivalamide 137281-08-4 C11H14N4O2
N-(4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-2-yl)pivalamide
—— 2,4-di(pyridin-4-yl)-1,3,5-triazine 39238-43-2 C13H9N5
2,4-di(pyridin-4-yl)-1,3,5-triazine
—— tert-butyl 4-cyano-4-(3,4-difluorophenyl)piperidine-1-carboxylate 906369-56-0 C17H20F2N2O2
tert-butyl 4-cyano-4-(3,4-difluorophenyl)piperidine-1-carboxylate
—— perfluoro(3-oxa-5-hexene)sulfonyl fluoride 67635-63-6 C5F10O3S
perfluoro(3-oxa-5-hexene)sulfonyl fluoride
—— 3-(3,5-dimethyl-1H-pyrazol-4-yl)propane-1-ol 1779428-05-5 C8H14N2O
3-(3,5-dimethyl-1H-pyrazol-4-yl)propane-1-ol
—— capmatinib acid 1029714-88-2 C22H14FN5O2
capmatinib acid
—— N-Benzylquinidinium chloride, 98% 77481-82-4 C27H31ClN2O2
N-Benzylquinidinium chloride, 98%
—— potassium 5-methyl-1,3,4-oxadiazole-2-carboxylate 888504-28-7 C4H3N2O3*K
potassium 5-methyl-1,3,4-oxadiazole-2-carboxylate
—— methyl 2-(2(((benzyloxy)carbonyl)amino)propan-2-yl)-5,6-dihydroxy-1,6-dihydropyrimidine-4-carboxylate 519032-08-7 C17H19N3O6
methyl 2-(2(((benzyloxy)carbonyl)amino)propan-2-yl)-5,6-dihydroxy-1,6-dihydropyrimidine-4-carboxylate
—— 3-Ethoxy-androsta-3,5-dien-17-on 972-46-3 C21H30O2
3-Ethoxy-androsta-3,5-dien-17-on