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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
—— 5'-O-Toluenesulphonyl-2'-deoxythymidine 7253-19-2 C17H20N2O7S
5'-O-Toluenesulphonyl-2'-deoxythymidine
—— 2-phenyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-ol 87753-08-0 C13H12N2O
2-phenyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-ol
—— PGD<sub>2</sub> 41598-07-6 C20H32O5
PGD<sub>2</sub>
—— 7β-[2-(thien-2-yl)acetamido]-3-hydroxymethyl-3-cephem-4-carboxylic acid 5935-65-9 C14H14N2O5S2
7β-[2-(thien-2-yl)acetamido]-3-hydroxymethyl-3-cephem-4-carboxylic acid
—— tris[2-(4-pyridyl)ethyl]phosphine oxide 131501-31-0 C21H24N3OP
tris[2-(4-pyridyl)ethyl]phosphine oxide
—— 5,6-diaminouracil hydrochloride 53608-89-2 C4H7ClN4O2
5,6-diaminouracil hydrochloride
—— 4,4'-Dichloroindigo 6275-44-1 C16H8Cl2N2O2
4,4'-Dichloroindigo
—— (R)-phenyl(pyridin-2-yl)methanol 5583-33-5 C12H11NO
(R)-phenyl(pyridin-2-yl)methanol
—— (-)-epipinoresinol 10061-38-8 C20H22O6
(-)-epipinoresinol
—— 1,4-diketo-3,6-bis(5-bromothienyl)pyrrolo[3,4-c]pyrrole 777079-55-7 C14H6Br2N2O2S2
1,4-diketo-3,6-bis(5-bromothienyl)pyrrolo[3,4-c]pyrrole
—— ethyl 4-(acetyloxy)-2-methyl-1-benzofuran-6-carboxylate 955886-29-0 C14H14O5
ethyl 4-(acetyloxy)-2-methyl-1-benzofuran-6-carboxylate
—— methyl 3-(methoxymethyl)-1H-pyrazole-4-carboxylate 318496-66-1 C7H10N2O3
methyl 3-(methoxymethyl)-1H-pyrazole-4-carboxylate
—— 5-bromo-3-methylindoline 86626-42-8 C9H10BrN
5-bromo-3-methylindoline
—— (R,R)-(+)-Weinsaeure-diethylester 87-91-2 C8H14O6
(R,R)-(+)-Weinsaeure-diethylester
—— 2-diethylamino-5-methanesulfonyl-benzoic acid 247569-56-8 C12H17NO4S
2-diethylamino-5-methanesulfonyl-benzoic acid
—— tert-butyl 4-(3-ethoxy-3-oxoprop-1-yn-1-yl)piperidine-1-carboxylate 203663-59-6 C15H23NO4
tert-butyl 4-(3-ethoxy-3-oxoprop-1-yn-1-yl)piperidine-1-carboxylate
—— 1,7-bis(tert-butyloxycarbonyl)-1,4,7,10-tetraazacyclododecane 913542-69-5 C18H36N4O4
1,7-bis(tert-butyloxycarbonyl)-1,4,7,10-tetraazacyclododecane
—— 2,5-dibromo-3-((2-(2-methoxyethoxy)ethoxy)methyl)thiophene 1048037-32-6 C10H14Br2O3S
2,5-dibromo-3-((2-(2-methoxyethoxy)ethoxy)methyl)thiophene
—— 4-carboxy-N-(4-carboxybutyl)phthalimide 115181-34-5 C14H13NO6
4-carboxy-N-(4-carboxybutyl)phthalimide
—— δ-valerobetaine 6778-33-2 C8H17NO2
δ-valerobetaine
—— (R,R)-QuinoxP 1107608-80-9 C18H28N2P2
(R,R)-QuinoxP
—— 2,2-dimethyl-3-[4-[5-[4-(trifluoromethyl)-1H-imidazol-2-yl]-2-pyridyl]phenoxy]propanoic acid 1382998-76-6 C20H18F3N3O3
2,2-dimethyl-3-[4-[5-[4-(trifluoromethyl)-1H-imidazol-2-yl]-2-pyridyl]phenoxy]propanoic acid
—— 3α-Brom-campher 76-29-9 C10H15BrO
3α-Brom-campher
—— Endo-α-bromocampher 76-29-9 C10H15BrO
Endo-α-bromocampher
—— 2-Hydroxycyclohexanessigsaeure 69198-05-6 C8H14O3
2-Hydroxycyclohexanessigsaeure
—— 4-amino-4-carboxypiperidine dihydrochloride 76508-73-1 C6H12N2O2*2ClH
4-amino-4-carboxypiperidine dihydrochloride
—— [5'-O-(4,4'-dimethoxytrityl)-N2-isobutyryl-2'-deoxyguanosine-3'-yl]-(N,N'-diisopropyl)methylphosphoramidite 84416-84-2 C42H53N6O8P
[5'-O-(4,4'-dimethoxytrityl)-N2-isobutyryl-2'-deoxyguanosine-3'-yl]-(N,N'-diisopropyl)methylphosphoramidite
—— 2,2'-(Buta-1,3-diene-1,4-diyl)dithiophene 23354-93-0 C12H10S2
2,2'-(Buta-1,3-diene-1,4-diyl)dithiophene
—— (E)-2-(1,3,3-trimethylindolin-2-ylidene)acetaldehyde 84-83-3 C13H15NO
(E)-2-(1,3,3-trimethylindolin-2-ylidene)acetaldehyde
—— 2-pyridineboronic acid N-phenyldiethanolamine ester 662138-96-7 C15H17BN2O2
2-pyridineboronic acid N-phenyldiethanolamine ester
—— ethyl 4-((2-ethoxy-3,4-dioxocyclobut-1-en-1-yl)-amino)-piperidine-1-carboxylate 933006-05-4 C14H20N2O5
ethyl 4-((2-ethoxy-3,4-dioxocyclobut-1-en-1-yl)-amino)-piperidine-1-carboxylate
—— N-{(1S)-1-[2-(1-{[(3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)-pyrrolidin-3-yl]carbonyl}piperidin-4-yl)-5-chlorophenyl]ethyl}acetamide 455956-93-1 C30H38ClF2N3O2
N-{(1S)-1-[2-(1-{[(3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)-pyrrolidin-3-yl]carbonyl}piperidin-4-yl)-5-chlorophenyl]ethyl}acetamide
—— 3-(4-bromophenyl)-1-methyl-1H-1,2,4-triazole 1184174-04-6 C9H8BrN3
3-(4-bromophenyl)-1-methyl-1H-1,2,4-triazole
—— 4-benzyl 1-tert-butyl 2-methylpiperazine-1,4-dicarboxylate 128102-16-9 C18H26N2O4
4-benzyl 1-tert-butyl 2-methylpiperazine-1,4-dicarboxylate
—— 2-bromo-5H-dibenzo[a,d][7]annulen-5-one 124853-22-1 C15H9BrO
2-bromo-5H-dibenzo[a,d][7]annulen-5-one
—— N,N’-dimethyl-2-phenyl-benzo[d]imidazolium iodide 3653-05-2 C15H15N2*I
N,N’-dimethyl-2-phenyl-benzo[d]imidazolium iodide
—— 2-(methylthio)-4,4-dimethyl-4,5-dihydro-1,3-oxazole 53244-68-1 C6H11NOS
2-(methylthio)-4,4-dimethyl-4,5-dihydro-1,3-oxazole
—— 1-(2,2,2-trifluoroethyl)piperazine dihydrochloride 13349-91-2 C6H11F3N2*2ClH
1-(2,2,2-trifluoroethyl)piperazine dihydrochloride
—— 6-benzyloxy-1,2,3,4-tetrahydro-isoquinoline 252061-94-2 C16H17NO
6-benzyloxy-1,2,3,4-tetrahydro-isoquinoline
—— 5-(3-methyl-5-(pyridin-4-yl)-4H-1,2,4-triazol-4-yl) isophthalic acid 1352638-29-9 C16H12N4O4
5-(3-methyl-5-(pyridin-4-yl)-4H-1,2,4-triazol-4-yl) isophthalic acid
—— 4,4'-bipyridine dihydrochloride 27926-72-3 C10H10N2*2Cl
4,4'-bipyridine dihydrochloride
—— 4-chloro-1-(4-nitrophenyl)-1H-pyrazole 65041-53-4 C9H6ClN3O2
4-chloro-1-(4-nitrophenyl)-1H-pyrazole
—— 10-methylphenothiazine radical cation 1207-72-3 C13H11NS
10-methylphenothiazine radical cation
—— 5-phenylresorcinol 7028-41-3 C12H10O2
5-phenylresorcinol
—— 1,1'-diheptyl-4,4'-bipyridinium dibromide 6159-05-3 2Br*C24H38N2
1,1'-diheptyl-4,4'-bipyridinium dibromide
—— 3-chloro-5-((6-oxo-1-((6-oxo-5-(trifluoromethyl)-1,6-dihydropyridazin-3-yl)methyl)-4-(trifluoromethyl)-1,6-dihydropyrimidin-5-yl)oxy)benzonitrile 1591823-76-5 C18H8ClF6N5O3
3-chloro-5-((6-oxo-1-((6-oxo-5-(trifluoromethyl)-1,6-dihydropyridazin-3-yl)methyl)-4-(trifluoromethyl)-1,6-dihydropyrimidin-5-yl)oxy)benzonitrile
—— 4-chloroacetophenone cyanohydrin 53066-09-4 C9H8ClNO
4-chloroacetophenone cyanohydrin
—— 3-bromo-4-[4-(4,6-dimethylpyrimidin-5-yl)-3-methylphenoxy]furo[3,2-c]pyridine 1609581-30-7 C20H16BrN3O2
3-bromo-4-[4-(4,6-dimethylpyrimidin-5-yl)-3-methylphenoxy]furo[3,2-c]pyridine
—— tert-butyl 6-methyl-4-(((trifluoromethyl)sulfonyl)oxy)-3,6-dihydropyridine-1(2H)-carboxylate 325488-26-4 C12H18F3NO5S
tert-butyl 6-methyl-4-(((trifluoromethyl)sulfonyl)oxy)-3,6-dihydropyridine-1(2H)-carboxylate
—— 7-Chloro-5-(4-fluorophenyl)thiazolo[4,5-d]pyrimidine 1043931-29-8 C11H5ClFN3S
7-Chloro-5-(4-fluorophenyl)thiazolo[4,5-d]pyrimidine