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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
—— 4-Bromo-5,8-dimethylquinoline 1070879-34-3 C11H10BrN
4-Bromo-5,8-dimethylquinoline
—— 4-Bromo-6,7-dichloroquinoline 1070879-39-8 C9H4BrCl2N
4-Bromo-6,7-dichloroquinoline
—— ZINC;12-hydroxyoctadec-9-enoate 13040-19-2 C36H66O6Zn
ZINC;12-hydroxyoctadec-9-enoate
—— 2-[2-[Carboxylatomethyl-[2-[carboxylatomethyl(carboxymethyl)amino]ethyl]amino]ethyl-(carboxymethyl)amino]-3-phenylmethoxypropanoate;gadolinium(3+);6-(methylamino)hexane-1,2,3,4,5-pentol 113662-23-0 C36H62GdN5O21
2-[2-[Carboxylatomethyl-[2-[carboxylatomethyl(carboxymethyl)amino]ethyl]amino]ethyl-(carboxymethyl)amino]-3-phenylmethoxypropanoate;gadolinium(3+);6-(methylamino)hexane-1,2,3,4,5-pentol
—— 1,5-Methano-11H-furo(3,2-g)pyrano(3,2-b)xanthene-3a(4H)-crotonaldehyde, 1,2,5,7-tetrahydro-8-hydroxy-alpha,2,2,11,11-pentamethyl-13-(3-methyl-2-butenyl)-4,7-dioxo-, trans- 1183-12-6 C33H36O7
1,5-Methano-11H-furo(3,2-g)pyrano(3,2-b)xanthene-3a(4H)-crotonaldehyde, 1,2,5,7-tetrahydro-8-hydroxy-alpha,2,2,11,11-pentamethyl-13-(3-methyl-2-butenyl)-4,7-dioxo-, trans-
—— momelotinib dimesylate 1056636-07-7 2CH4O3S*C23H22N6O2
momelotinib dimesylate
—— (2S)-1-[(Benzyloxy)carbonyl]azetidine-2-carboxylate 25654-52-8 C12H12NO4-
(2S)-1-[(Benzyloxy)carbonyl]azetidine-2-carboxylate
—— copper;quinolin-8-ol 13014-03-4 2C9H7NO*Cu
copper;quinolin-8-ol
—— 2-(Pyrimidin-5-yl)ethanamine 856973-36-9 C6H9N3
2-(Pyrimidin-5-yl)ethanamine
—— Di(p-tolylidene)sorbitol 54686-97-4 C22H26O6
Di(p-tolylidene)sorbitol
—— (2S,3R,5R)-5-Chloro-2-(((4-chlorobenzoyl)oxy)methyl)tetrahydrofuran-3-yl 4-chlorobenzoate 21740-23-8 C19H15Cl3O5
(2S,3R,5R)-5-Chloro-2-(((4-chlorobenzoyl)oxy)methyl)tetrahydrofuran-3-yl 4-chlorobenzoate
—— 2-Picolineborane 3999-38-0 C6H7BN
2-Picolineborane
—— 2-cyclopropylpyridin-4-amine 340006-71-5 C8H10N2
2-cyclopropylpyridin-4-amine
—— (1R,3s,5S)-8-Benzyl-3-(3-isopropyl-5-methyl-4H-1,2,4-triazol-4-yl)-8-azabicyclo[3.2.1]octane 423165-13-3 C20H28N4
(1R,3s,5S)-8-Benzyl-3-(3-isopropyl-5-methyl-4H-1,2,4-triazol-4-yl)-8-azabicyclo[3.2.1]octane
—— magnesium;3H-pyridin-3-ide;bromide 21970-14-9 C5H4BrMgN
magnesium;3H-pyridin-3-ide;bromide
—— 3-(Quinolin-6-YL)propan-1-amine 465529-51-5 C12H14N2
3-(Quinolin-6-YL)propan-1-amine
—— 3-(1-H-imidazol-4-yl)propanol 49549-75-9 C6H10N2O
3-(1-H-imidazol-4-yl)propanol
—— 7-chloroisoquinoline-1(2H)-thione 130874-99-6 C9H6ClNS
7-chloroisoquinoline-1(2H)-thione
—— 2-Bromo-5-(1-methyl-azetidin-3-yloxy)-pyridine 1242156-74-6 C9H11BrN2O
2-Bromo-5-(1-methyl-azetidin-3-yloxy)-pyridine
—— 2-isopropyl-4-(((N-methyl)amino)methyl)thiazole dihydrochloride 1185167-55-8 C8H14N2S*2ClH
2-isopropyl-4-(((N-methyl)amino)methyl)thiazole dihydrochloride
—— N-methyl-N-(2-pyridyl)acrylamide 1156926-11-2 C9H10N2O
N-methyl-N-(2-pyridyl)acrylamide
—— 4-bromomethyl-3-chloro-benzamide 3932-97-6 C8H7BrClNO
4-bromomethyl-3-chloro-benzamide
—— ((3SR,4SR)-1-tert-butoxycarbonyl)4-(ethoxycarbonyl)pyrrolidine-3-carboxylic acid 252919-44-1 C13H21NO6
((3SR,4SR)-1-tert-butoxycarbonyl)4-(ethoxycarbonyl)pyrrolidine-3-carboxylic acid
—— 1-(5-methylpyridin-2-yl)piperidine-4-carboxylic acid 954576-20-6 C12H16N2O2
1-(5-methylpyridin-2-yl)piperidine-4-carboxylic acid
—— 1,3,5-CYCLOHEXANETRICARBONITRILE 168280-46-4 C9H9N3
1,3,5-CYCLOHEXANETRICARBONITRILE
—— pyridine-2-carboxylic acid, Ag(II) salt 14783-00-7 C12H8AgN2O4
pyridine-2-carboxylic acid, Ag(II) salt
—— Cinchonine sulfate 5949-16-6 C38H46N4O6S
Cinchonine sulfate
—— Aerobid 77326-96-6 C48H64F2O13
Aerobid
—— [3H]-(–)-2-b-carbomethoxy-3-b-(4-fluorophenyl)tropane. 50370-56-4 C16H20FNO2
[3H]-(–)-2-b-carbomethoxy-3-b-(4-fluorophenyl)tropane.
—— 1,2-difluoro-3-((4-fluoro-2-methoxy-5-nitrophenoxy)methyl)-4-methoxybenzene 1073435-71-8 C15H12F3NO5
1,2-difluoro-3-((4-fluoro-2-methoxy-5-nitrophenoxy)methyl)-4-methoxybenzene
—— methyl 4-[2-(2-amino-4,7-dihydro-4-oxo-1H-pyrrole[2,3-d]pyrimidin-5-yl)ethyl]benzoate 155405-80-4 C16H16N4O3
methyl 4-[2-(2-amino-4,7-dihydro-4-oxo-1H-pyrrole[2,3-d]pyrimidin-5-yl)ethyl]benzoate
—— ethyl-3,1-(2,4-difluoroanilino)-2-(2,6-dichloro-5-fluoronicotinyl) acrylate 100490-99-1 C17H11Cl2F3N2O3
ethyl-3,1-(2,4-difluoroanilino)-2-(2,6-dichloro-5-fluoronicotinyl) acrylate
—— phenyl 2-O-benzyl-4,6-O-benzylidene-3-O-p-methoxybenzyl-1-thio-α-D-mannopyranoside 177943-74-7 C34H34O6S
phenyl 2-O-benzyl-4,6-O-benzylidene-3-O-p-methoxybenzyl-1-thio-α-D-mannopyranoside
—— 2-chloropyrido[2,3-d]pyrimidin-4(3H)-one 93049-38-8 C7H4ClN3O
2-chloropyrido[2,3-d]pyrimidin-4(3H)-one
—— 1-hydroxymethyl-1-phenylcyclopentane 59115-90-1 C12H16O
1-hydroxymethyl-1-phenylcyclopentane
—— 2,7-diacetylfluorenone 39665-89-9 C17H12O3
2,7-diacetylfluorenone
—— methyl 8-hydroxyquinoline-4-carboxylate 71294-66-1 C11H9NO3
methyl 8-hydroxyquinoline-4-carboxylate
—— p-methoxyphenyl 2,3,6-tri-O-benzyl-β-D-galactopyranoside 869107-36-8 C34H36O7
p-methoxyphenyl 2,3,6-tri-O-benzyl-β-D-galactopyranoside
—— benzhydryl 3-hydroxy-7β-(α-phenylacetamido)-3-cephem-4-carboxylate 54639-48-4 C28H24N2O5S
benzhydryl 3-hydroxy-7β-(α-phenylacetamido)-3-cephem-4-carboxylate
—— Koenigin 20186-29-2 C16H18O9
Koenigin
—— 7-(6-fluoropyridin-3-yl)-5H-pyrido[4,3-b]indole 1415379-56-4 C16H10FN3
7-(6-fluoropyridin-3-yl)-5H-pyrido[4,3-b]indole
—— 4,5-bis(2-methoxyethoxy)benzene-1,2-diamine 344438-55-7 C12H20N2O4
4,5-bis(2-methoxyethoxy)benzene-1,2-diamine
—— (R)-1-((S)-tert-butylsulfinyl)-2-(2,5-difluorophenyl)pyrrolidine 1443538-31-5 C14H19F2NOS
(R)-1-((S)-tert-butylsulfinyl)-2-(2,5-difluorophenyl)pyrrolidine
—— ((3aR,5R,6S,6aR)-5-((tert-butyldiphenylsilyloxy)methyl)-2,2-dimethyl-6-(naphthalen-2-ylmethoxy)-dihydro-5H-furo[3,2-d][1,3]dioxol-5-yl)methanol 956485-08-8 C36H42O6Si
((3aR,5R,6S,6aR)-5-((tert-butyldiphenylsilyloxy)methyl)-2,2-dimethyl-6-(naphthalen-2-ylmethoxy)-dihydro-5H-furo[3,2-d][1,3]dioxol-5-yl)methanol
—— 6-(dimethylamino)-2H-chromen-2-one 98786-08-4 C11H11NO2
6-(dimethylamino)-2H-chromen-2-one
—— (S)-Viloxazine Hydrochloride 56287-61-7 C13H20ClNO3
(S)-Viloxazine Hydrochloride
—— pyrimidine 1,3-dioxide 56642-54-7 C4H4N2O2
pyrimidine 1,3-dioxide
—— 2-benzyloxycarbonyl-3-ethyl-4-methylpyrrole 5866-56-8 C15H17NO2
2-benzyloxycarbonyl-3-ethyl-4-methylpyrrole
—— Morpholine, 2-[[2-(ethoxy-d5)phenoxy]methyl]- 117320-32-8 C13H19NO3
Morpholine, 2-[[2-(ethoxy-d5)phenoxy]methyl]-
—— α-(4-pyridyl-1-oxide)-N-t-butylnitrone 66893-81-0 C10H14N2O2
α-(4-pyridyl-1-oxide)-N-t-butylnitrone