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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
—— 2-amino-4-(2,3-dimethoxyphenyl)-butanoic acid hydrochloride 149060-64-0 C12H17NO4*ClH
2-amino-4-(2,3-dimethoxyphenyl)-butanoic acid hydrochloride
—— pyrazine(bis)trifluoroborane 34038-18-1 C4H4B2F6N2
pyrazine(bis)trifluoroborane
—— (2S)-2-phenyl-2-[(2R)-piperidin-2-yl]acetic acid;hydrochloride 19130-92-8 C13H18ClNO2
(2S)-2-phenyl-2-[(2R)-piperidin-2-yl]acetic acid;hydrochloride
—— (Z)-((1,1,1,5,5,5-hexafluoro-4-oxopent-2-en-2-yl)oxy)iridium,(1Z,5Z)-cycloocta-1,5-diene 34801-95-1 C13H14F6IrO2
(Z)-((1,1,1,5,5,5-hexafluoro-4-oxopent-2-en-2-yl)oxy)iridium,(1Z,5Z)-cycloocta-1,5-diene
—— (N-{phenyl[2-(pyridine-2-carboxamido)phenyl]methylidene}glycinato-N,N',N'',O)nickel(II) 124302-98-3 C21H15N3NiO3
(N-{phenyl[2-(pyridine-2-carboxamido)phenyl]methylidene}glycinato-N,N',N'',O)nickel(II)
—— 6-Iodo-1-(oxan-2-yl)-3-[2-(pyridin-2-yl)ethenyl]-1H-indazole 886230-77-9 C19H18IN3O
6-Iodo-1-(oxan-2-yl)-3-[2-(pyridin-2-yl)ethenyl]-1H-indazole
—— 2’-deoxyuridine 5’-monophosphate disodium salt 42155-08-8 C9H11N2O8P*2Na
2’-deoxyuridine 5’-monophosphate disodium salt
—— Sodium;4-[[4-(diethylamino)phenyl]diazenyl]benzenesulfonic acid;hydride 13545-67-0 C16H20N3NaO3S
Sodium;4-[[4-(diethylamino)phenyl]diazenyl]benzenesulfonic acid;hydride
—— [1,1':4',1''-terphenyl]-2,2''-dicarbaldehyde 1334652-46-8 C20H14O2
[1,1':4',1''-terphenyl]-2,2''-dicarbaldehyde
—— [(E)-[(3R,4R,5S,6R)-3-acetamido-4,5-dihydroxy-6-(hydroxymethyl)oxan-2-ylidene]amino] N-(2,3,4,5,6-pentadeuteriophenyl)carbamate 1331383-16-4 C15H19N3O7
[(E)-[(3R,4R,5S,6R)-3-acetamido-4,5-dihydroxy-6-(hydroxymethyl)oxan-2-ylidene]amino] N-(2,3,4,5,6-pentadeuteriophenyl)carbamate
—— trans-4-t-butylcyclohexylamine 2163-34-0 C10H21N
trans-4-t-butylcyclohexylamine
—— methyl trans-1-oxaspiro[2.3]hexane-5-carboxylate 578715-80-7 C7H10O3
methyl trans-1-oxaspiro[2.3]hexane-5-carboxylate
—— Olaparib monohydrate 2093369-28-7 C24H25FN4O4
Olaparib monohydrate
—— 5-iodo-4-methyl-7H-pyrrolo[2,3-d]pyrimidine 1303426-83-6 C7H6IN3
5-iodo-4-methyl-7H-pyrrolo[2,3-d]pyrimidine
—— 4-chloro-2,3-dihydro-1H-pyrrolo[2,3-b]pyridine 1354454-95-7 C7H7ClN2
4-chloro-2,3-dihydro-1H-pyrrolo[2,3-b]pyridine
—— methyl 4-chloro-1-tosyl-1H-pyrrolo[2,3-b]pyridine-5-carboxylate 1374243-51-2 C16H13ClN2O4S
methyl 4-chloro-1-tosyl-1H-pyrrolo[2,3-b]pyridine-5-carboxylate
—— 4-Chloro-5-methoxyquinoline 1231761-14-0 C10H8ClNO
4-Chloro-5-methoxyquinoline
—— 5’-O-Trityl-3’-β-hydroxythymidine 7791-71-1 C29H28N2O5
5’-O-Trityl-3’-β-hydroxythymidine
—— 3,7-dichloro-5,5-dimethyl-5H-dibenzo[b,d]silole 1252259-63-4 C14H13ClSi
3,7-dichloro-5,5-dimethyl-5H-dibenzo[b,d]silole
—— trans-4-amino-trans-2-methylcyclohexanol 1314963-60-4 C7H15NO
trans-4-amino-trans-2-methylcyclohexanol
—— methyl 2-amino-5-iodo-thiazole-4-carboxylate 1235034-76-0 C5H5IN2O2S
methyl 2-amino-5-iodo-thiazole-4-carboxylate
—— ((1R,8S,9s)-bicyclo[6.1.0]non-4-en-9-yl)methanol 374898-56-3 C10H16O
((1R,8S,9s)-bicyclo[6.1.0]non-4-en-9-yl)methanol
—— trans-3-tert-Butoxycarbonylaminocyclohex-4-enecarboxylic acid 1008773-81-6 C12H19NO4
trans-3-tert-Butoxycarbonylaminocyclohex-4-enecarboxylic acid
—— bis(2-phenylpyridinato)(2,2'-bipyridine)iridium(III) hexafluorophosphate 106294-60-4 C32H24IrN4*F6P
bis(2-phenylpyridinato)(2,2'-bipyridine)iridium(III) hexafluorophosphate
—— t-butyl 3-(4-iodo-1H-pyrazol-1-yl)azetidine-1-carboxylate 951259-19-1 C11H16IN3O2
t-butyl 3-(4-iodo-1H-pyrazol-1-yl)azetidine-1-carboxylate
—— N2-[[1-(9H-Fluoren-9-yl)ethoxy]carbonyl]-D-glutamine 118609-68-0 C21H22N2O5
N2-[[1-(9H-Fluoren-9-yl)ethoxy]carbonyl]-D-glutamine
—— Fmoc-Leucine,NCA 125814-21-3 C22H21NO5
Fmoc-Leucine,NCA
—— N-nitrosoenalapril 2994317-06-3 C20H27N3O6
N-nitrosoenalapril
—— 2-oxa-7-azaspiro[4.4]nonan-8-one 1384427-76-2 C7H11NO2
2-oxa-7-azaspiro[4.4]nonan-8-one
—— 2-Chloro-5-cyclopropylpyrazine 1244761-68-9 C7H7ClN2
2-Chloro-5-cyclopropylpyrazine
—— 2-(triphenylsilyl)-9H-carbazole 1262866-95-4 C30H23NSi
2-(triphenylsilyl)-9H-carbazole
—— 3-chloro-5-methoxyisoquinoline 1691715-12-4 C10H8ClNO
3-chloro-5-methoxyisoquinoline
—— 4-(6-methyl-1,2,4,5-tetrazin-3-yl)phenol 58884-35-8 C9H8N4O
4-(6-methyl-1,2,4,5-tetrazin-3-yl)phenol
—— 2-(2-Methyl-1-piperidinyl)isonicotinic acid 1019127-10-6 C12H16N2O2
2-(2-Methyl-1-piperidinyl)isonicotinic acid
—— Tris[4,4'-bis(t-butyl)-2,2'-bipyridine]ruthenium(II) hexafluorophosphate 75777-87-6 C54H72N6Ru+2
Tris[4,4'-bis(t-butyl)-2,2'-bipyridine]ruthenium(II) hexafluorophosphate
—— 5-chloro-2,3,3-trimethyl-3H-pyrrolo[2,3-b]pyridine 596085-87-9 C10H11ClN2
5-chloro-2,3,3-trimethyl-3H-pyrrolo[2,3-b]pyridine
—— tropine-3-thiol hydrochloride 1141886-66-9 C8H15NS*ClH
tropine-3-thiol hydrochloride
—— Δ<sup>1,4</sup>-16α-Methyl-6α,9α-difluoro-11β,17α-dihydroxy-3-oxo-androstadien-17-carbonsaeuremethylester 28416-84-4 C22H28F2O5
Δ<sup>1,4</sup>-16α-Methyl-6α,9α-difluoro-11β,17α-dihydroxy-3-oxo-androstadien-17-carbonsaeuremethylester
—— Elsubrutinib 1643570-24-4 C17H19N3O2
Elsubrutinib
—— N,N′-bis(2,6-bis(diphenylmethyl)-4-methoxyphenyl)imidazol-2-ylidenium chloride 1416368-03-0 C69H57N2O2*Cl
N,N′-bis(2,6-bis(diphenylmethyl)-4-methoxyphenyl)imidazol-2-ylidenium chloride
—— (1R)-((2S,4S,5R)-5-ethylquinuclidin-2-yl)(6-methoxyquinolin-4-yl)methanol hydrochloride 1476-98-8 C20H26N2O2*ClH
(1R)-((2S,4S,5R)-5-ethylquinuclidin-2-yl)(6-methoxyquinolin-4-yl)methanol hydrochloride
—— tert-butyl[(1S)-3-iodo-1-phenethylpropyl]oxydimethylsilane 876953-73-0 C17H29IOSi
tert-butyl[(1S)-3-iodo-1-phenethylpropyl]oxydimethylsilane
—— ethyl 6-bromo-[1,2,4]triazolo[1,5-a]pyridine-2-carboxylate 1427376-40-6 C9H8BrN3O2
ethyl 6-bromo-[1,2,4]triazolo[1,5-a]pyridine-2-carboxylate
—— 2-Methylheptyl 8-methylnonyl benzene-1,2-dicarboxylate 94770-75-9 C26H42O4
2-Methylheptyl 8-methylnonyl benzene-1,2-dicarboxylate
—— (3-Fluoropiperidin-3-yl)methanol hydrochloride 1416440-21-5 C6H13ClFNO
(3-Fluoropiperidin-3-yl)methanol hydrochloride
—— bromozinc(1+),6-methoxy-2H-pyridin-2-ide 352530-39-3 C6H6BrNOZn
bromozinc(1+),6-methoxy-2H-pyridin-2-ide
—— Acefylline piperazine 18833-13-1 C22H30N10O8
Acefylline piperazine
—— 3-(tert-butoxycarbonyl)-4,4,4-trifluorobutanoic acid 1185296-42-7 C9H14F3NO4
3-(tert-butoxycarbonyl)-4,4,4-trifluorobutanoic acid
—— [Os4(CO)12(μ-H)4] 12375-04-1 C12H4O12Os4
[Os4(CO)12(μ-H)4]
—— 2,4,7-trichloro[2,3-d]pyrimidine-6-carbonitrile 117506-01-1 C8HCl3N4
2,4,7-trichloro[2,3-d]pyrimidine-6-carbonitrile