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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
—— thietane-3-carbonitrile 1337882-54-8 C4H5NS
thietane-3-carbonitrile
—— 4-nornicotine 130343-15-6 C9H12N2
4-nornicotine
—— 2-((3bS,4aR)-5,5-difluoro-3-(trifluoromethyl)-3b,4,4a,5-tetrahydro-1H-cyclopropa[3,4]cyclopenta[1,2-c]pyrazol-1-yl)acetic acid 1620056-83-8 C10H7F5N2O2
2-((3bS,4aR)-5,5-difluoro-3-(trifluoromethyl)-3b,4,4a,5-tetrahydro-1H-cyclopropa[3,4]cyclopenta[1,2-c]pyrazol-1-yl)acetic acid
—— 3-bromo-8-chloro-2-(trifluoromethyl)imidazo[1,2-a]pyrazine 1334167-29-1 C7H2BrClF3N3
3-bromo-8-chloro-2-(trifluoromethyl)imidazo[1,2-a]pyrazine
—— trans-2-methyltetrahydropyran-4-ol 55230-32-5 C6H12O2
trans-2-methyltetrahydropyran-4-ol
—— cis-2-methyl-4-pyranol 33747-08-9 C6H12O2
cis-2-methyl-4-pyranol
—— d-menthyl glyoxalate monohydrate 111969-64-3 C12H22O4
d-menthyl glyoxalate monohydrate
—— N-methoxy-N,1-dimethyl-1H-pyrazol-5-carboxamide 1339452-16-2 C7H11N3O2
N-methoxy-N,1-dimethyl-1H-pyrazol-5-carboxamide
—— 5-Bromo-2-((4-methylpiperidin-1-YL)sulfonyl)pyridine 912934-64-6 C11H15BrN2O2S
5-Bromo-2-((4-methylpiperidin-1-YL)sulfonyl)pyridine
—— 7-isopropyl-quinoline 74525-47-6 C12H13N
7-isopropyl-quinoline
—— (S)-tert-butyl 4-bromo-2,3-dihydro-1H-inden-1-ylcarbamate 1307231-21-5 C14H18BrNO2
(S)-tert-butyl 4-bromo-2,3-dihydro-1H-inden-1-ylcarbamate
—— BTRX-335140 2244614-14-8 C25H32FN5O2
BTRX-335140
—— (1S,4S)-2-azabicyclo[2.2.1]hept-5-en-3-one 130931-83-8 C6H7NO
(1S,4S)-2-azabicyclo[2.2.1]hept-5-en-3-one
—— (1S)-(+)-2-Azabicyclo[2.2.1]hept-5-en-3-one 130931-83-8 C6H7NO
(1S)-(+)-2-Azabicyclo[2.2.1]hept-5-en-3-one
—— (2E)-3-(1H-indol-3-yl)prop-2-enoate 1204-06-4 C11H8NO2-
(2E)-3-(1H-indol-3-yl)prop-2-enoate
—— N-(6-(6-chloro-5-(4-fluorophenylsulfonamido)pyridin-3-yl)imidazo[1,2-b]pyridazin-2-yl)acetamide 1162680-13-8 C19H14ClFN6O3S
N-(6-(6-chloro-5-(4-fluorophenylsulfonamido)pyridin-3-yl)imidazo[1,2-b]pyridazin-2-yl)acetamide
—— Ammonium (Z)-alpha-methoxyimino-2-furylacetate 97148-39-5 C7H6NO4-
Ammonium (Z)-alpha-methoxyimino-2-furylacetate
—— 2-(1-piperazinyl)quinoline hydrochloride 928026-67-9 C13H15N3*ClH
2-(1-piperazinyl)quinoline hydrochloride
—— 4-Chloro-1-benzothiophene-2-carboxylate 23967-57-9 C9H4ClO2S-
4-Chloro-1-benzothiophene-2-carboxylate
—— 2,6,8-Trimethylquinoline-4-carboxylate 93189-20-9 C13H12NO2-
2,6,8-Trimethylquinoline-4-carboxylate
—— (5-nitro-1H-1,2,4-triazol-3-yl)acetic acid 173167-32-3 C4H4N4O4
(5-nitro-1H-1,2,4-triazol-3-yl)acetic acid
—— 4-nitro-2,6-bis(pyrrolidin-1'-ylmethyl)phenol 121836-29-1 C16H23N3O3
4-nitro-2,6-bis(pyrrolidin-1'-ylmethyl)phenol
—— 2,3-norbornanediol 14440-78-9 C7H12O2
2,3-norbornanediol
—— (S)-3-amino-4,4,4-trifluorobutanoic acid 151871-99-7 C4H6F3NO2
(S)-3-amino-4,4,4-trifluorobutanoic acid
—— 1-acetyl-(E)-3-benzylidene-2,5-piperazinedione 30166-29-1 C13H12N2O3
1-acetyl-(E)-3-benzylidene-2,5-piperazinedione
—— 2,4-Distyrylphenol 2012-21-7 C22H18O
2,4-Distyrylphenol
—— [(6Z,10Z)-9-acetyloxy-6,10-dimethyl-3-methylidene-2-oxo-3a,4,5,8,9,11a-hexahydrocyclodeca[b]furan-4-yl] (E)-4-hydroxy-2-(hydroxymethyl)but-2-enoate 38458-58-1 C22H28O8
[(6Z,10Z)-9-acetyloxy-6,10-dimethyl-3-methylidene-2-oxo-3a,4,5,8,9,11a-hexahydrocyclodeca[b]furan-4-yl] (E)-4-hydroxy-2-(hydroxymethyl)but-2-enoate
—— methyl (2E)-1,3,3-trimethyl-2-[(2Z)-2-(3-methyl-5-oxo-1-phenylpyrazol-4-ylidene)ethylidene]indole-6-carboxylate 5718-26-3 C25H25N3O3
methyl (2E)-1,3,3-trimethyl-2-[(2Z)-2-(3-methyl-5-oxo-1-phenylpyrazol-4-ylidene)ethylidene]indole-6-carboxylate
—— 2-(4-chlorophenyl)pyrimidine-5-carboxylic acid 878691-37-3 C11H7ClN2O2
2-(4-chlorophenyl)pyrimidine-5-carboxylic acid
—— 1,3,3-trimethyl-6'-nitrospiro(indoline-2,2'-<2H-1>benzothiopyran) 85000-11-9 C19H18N2O2S
1,3,3-trimethyl-6'-nitrospiro(indoline-2,2'-<2H-1>benzothiopyran)
—— Neoglucobrassicin 5187-84-8 C17H22N2O10S2
Neoglucobrassicin
—— (R)-(+)-trans-4-(1-Aminoethyl)-N-(4-Pyridyl)cyclohexanecarboxamide dihydrochloride monohydrate 331752-47-7 C14H25Cl2N3O2
(R)-(+)-trans-4-(1-Aminoethyl)-N-(4-Pyridyl)cyclohexanecarboxamide dihydrochloride monohydrate
—— ONT 093 216227-54-2 C32H38N4O
ONT 093
—— ethyl 2-cyclobutyl-2-oxoacetate 861160-59-0 C8H12O3
ethyl 2-cyclobutyl-2-oxoacetate
—— fluoromethylhexahydropyridine 886216-73-5 C6H12FN
fluoromethylhexahydropyridine
—— 2-bromo-4-phenylpyrimidine 10198-98-8 C10H7BrN2
2-bromo-4-phenylpyrimidine
—— 2,6-dibromo-3-nitro-toluene 110127-07-6 C7H5Br2NO2
2,6-dibromo-3-nitro-toluene
—— 5-bromo-2-chloro-3-fluoromethyl-pyridine 1335052-20-4 C6H4BrClFN
5-bromo-2-chloro-3-fluoromethyl-pyridine
—— 3beta-Acetoxy-5alpha-pregn-16-en-20-one 1169-20-6 C23H34O3
3beta-Acetoxy-5alpha-pregn-16-en-20-one
—— 3-(6-Trifluoromethyl-3-pyridinyl)-2-propenoic acid 773131-93-4 C9H6F3NO2
3-(6-Trifluoromethyl-3-pyridinyl)-2-propenoic acid
—— 11α-Acetoxy-pregnen-(4)-dion-(3,20) 2268-98-6 C23H32O4
11α-Acetoxy-pregnen-(4)-dion-(3,20)
—— 4-(3-chlorophenyl)-2,6-diphenylpyridine 83993-80-0 C23H16ClN
4-(3-chlorophenyl)-2,6-diphenylpyridine
—— (2S,3S)-3-methoxy-pyrrolidine-1,2-dicarboxylic acid 1-(9H-fluoren-9-ylmethyl) ester 1344157-79-4 C21H21NO5
(2S,3S)-3-methoxy-pyrrolidine-1,2-dicarboxylic acid 1-(9H-fluoren-9-ylmethyl) ester
—— N'-(6,7-methylenedioxyquinolin-4-yl)-N,N-dimethylethane-1,2-diamine 500214-39-1 C14H17N3O2
N'-(6,7-methylenedioxyquinolin-4-yl)-N,N-dimethylethane-1,2-diamine
—— 1-benzo[<i>b</i>]thiophen-3-yl-3-dimethylamino-propan-1-one; hydrochloride 61-40-5 C13H15NOS*ClH
1-benzo[<i>b</i>]thiophen-3-yl-3-dimethylamino-propan-1-one; hydrochloride
—— 2-(2,3-dihydrobenzofuran-7-yl)acetonitrile 485828-88-4 C10H9NO
2-(2,3-dihydrobenzofuran-7-yl)acetonitrile
—— Convallatoxin 508-75-8 C29H42O10
Convallatoxin
—— Corglykon 508-75-8 C29H42O10
Corglykon
—— methyl 3,5-di-O-benzyl-D-xylofuranoside 102339-30-0 C20H24O5
methyl 3,5-di-O-benzyl-D-xylofuranoside
—— epinodosin 10391-09-0 C20H26O6
epinodosin