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原料药中间体

原料药中间体是指在药物合成过程中用于生成最终活性成分(即原料药)的化学物质。这些中间体在制药工业中扮演着重要角色,它们通过一系列化学反应逐步转化成成品药物。根据其在生产过程中的位置和功能,可以将原料药中间体分为以下几个类别:

  1. 起始物料:这类中间体是最初用于合成最终产品的原材料。它们通常来源于天然产物、化工产品或其他已经存在的化合物。

  2. 关键中间体:这些中间体在整个合成过程中起着核心作用,通常是通过复杂的化学反应得到的。它们对于确保原料药的质量和成本效益至关重要。

  3. 保护基团:在药物合成中使用这类中间体是为了对某些敏感部分进行临时性或选择性的“保护”,防止它们在不必要的位置上发生副反应。保护完成后可通过特定条件去除这些保护基。

  4. 催化剂和添加剂:虽然不直接形成最终产品,但这些物质能够促进化学反应、提高产率或改善产品的质量特性。

  5. 分离纯化溶剂:这类中间体主要用于原料药合成过程中的提纯步骤。它们帮助从目标产物中去除杂质并提高产品的纯度。

选择合适的原料药中间体对于保证药物的安全性和有效性至关重要,因此,在其开发过程中需要考虑多个因素,包括成本效益、反应条件的可控性以及环境友好型等方面。

下级分类

中文名称 英文名称 CAS号 化学式 结构式图片
—— N,N'-Dicarbobenzoxy-L-β-lysin 35107-12-1 C22H26N2O6
N,N'-Dicarbobenzoxy-L-β-lysin
—— 2'-O-[2-(methylamino)-2-oxoethyl]-5-methyluridine 815632-50-9 C13H19N3O7
2'-O-[2-(methylamino)-2-oxoethyl]-5-methyluridine
—— 2-aminocyclohexanecarboxamide 34126-95-9 C7H14N2O
2-aminocyclohexanecarboxamide
—— 7-amino-3-hydroxycepham-4-carboxylic acid 68403-70-3 C7H10N2O4S
7-amino-3-hydroxycepham-4-carboxylic acid
—— (Z,2R)-5-amino-2-(dibenzylamino)-1,6-diphenylhex-4-en-3-one 156732-13-7 C32H32N2O
(Z,2R)-5-amino-2-(dibenzylamino)-1,6-diphenylhex-4-en-3-one
—— 3-<(tert-Butoxycarbonyl)amino>-4-hydroxy-L-butyric acid 83345-44-2 C9H17NO5
3-<(tert-Butoxycarbonyl)amino>-4-hydroxy-L-butyric acid
—— (Z)-2-(hydroxyimino)-6-methoxy-2,3-dihydro-1H-inden-1-one 24077-98-3 C10H9NO3
(Z)-2-(hydroxyimino)-6-methoxy-2,3-dihydro-1H-inden-1-one
—— (S)-(-)-Blebbistatin O-Benzoate 1217832-61-5 C25H20N2O3
(S)-(-)-Blebbistatin O-Benzoate
—— (S,E)-4,8-dimethylnona-3,7-dien-2-ol 67845-50-5 C11H20O
(S,E)-4,8-dimethylnona-3,7-dien-2-ol
—— ellipticine quinone 73326-98-4 C15H8N2O2
ellipticine quinone
—— (S)-α-methylserine hydrochloride 114396-62-2 C4H9NO3*ClH
(S)-α-methylserine hydrochloride
—— 4'-(bromomethyl)-N-(4,5-dimethyl-3-isoxazolyl)-2'-(ethoxymethyl)-N-(methoxymethyl) [1,1'-biphenyl]-2-sulfonamide 1026273-26-6 C23H27BrN2O5S
4'-(bromomethyl)-N-(4,5-dimethyl-3-isoxazolyl)-2'-(ethoxymethyl)-N-(methoxymethyl) [1,1'-biphenyl]-2-sulfonamide
—— 4'-[(2-butyl-4-oxo-1,3-diazaspiro[4.4]non-1-en-3-yl)methyl-N-](4,5-dimethyl-3-isoxazolyl)-2'-(ethoxymethyl)-N-(methoxymethyl) [1,1'-biphenyl]-2-sulfonamide 1026355-73-6 C34H44N4O6S
4'-[(2-butyl-4-oxo-1,3-diazaspiro[4.4]non-1-en-3-yl)methyl-N-](4,5-dimethyl-3-isoxazolyl)-2'-(ethoxymethyl)-N-(methoxymethyl) [1,1'-biphenyl]-2-sulfonamide
—— tert-butyl (3S)-3-[methoxy(methyl)carbamoyl]pyrrolidine-1-carboxylate 1204677-53-1 C12H22N2O4
tert-butyl (3S)-3-[methoxy(methyl)carbamoyl]pyrrolidine-1-carboxylate
—— 3-hydroxy-5-methoxybenzonitrile 124993-53-9 C8H7NO2
3-hydroxy-5-methoxybenzonitrile
—— tert-butyl 2'-oxospiro[azetidine-3,3'-indoline]-1-carboxylate 1251001-73-6 C15H18N2O3
tert-butyl 2'-oxospiro[azetidine-3,3'-indoline]-1-carboxylate
—— 1-Phenyl-3-<2-phenylmercapto-aethyl>-thioharnstoff 13084-43-0 C15H16N2S2
1-Phenyl-3-<2-phenylmercapto-aethyl>-thioharnstoff
—— 5endo-Brommethyl-2-norbornen 16002-25-8 C8H11Br
5endo-Brommethyl-2-norbornen
—— (S)-2-amino-6-((4-methoxyphenyl)diphenylmethyl-amino)hexanoic acid 159857-61-1 C26H30N2O3
(S)-2-amino-6-((4-methoxyphenyl)diphenylmethyl-amino)hexanoic acid
—— (10S,13S)-17-Acetyl-10,13-dimethyl-6,7,8,10,12,13,14,15-octahydro-cyclopenta[a]phenanthren-3-one 117048-56-3 C21H24O2
(10S,13S)-17-Acetyl-10,13-dimethyl-6,7,8,10,12,13,14,15-octahydro-cyclopenta[a]phenanthren-3-one
—— 21-Acetoxy-1,4,9(11),16-pregnatetraen-3,20-dion 37413-91-5 C23H26O4
21-Acetoxy-1,4,9(11),16-pregnatetraen-3,20-dion
—— tert-butyl (4S)-5-amino-4-(benzyloxycarbonylamino)-5-oxopentanoate 17191-52-5 C17H24N2O5
tert-butyl (4S)-5-amino-4-(benzyloxycarbonylamino)-5-oxopentanoate
—— 3-azabicyclo[3.3.0]octane hydrochloride 112626-50-3 C7H13N*ClH
3-azabicyclo[3.3.0]octane hydrochloride
—— 1,8-dibromo-octane-2,7-dione 39095-41-5 C8H12Br2O2
1,8-dibromo-octane-2,7-dione
—— benzyl 2-acetamido-2-deoxy-3,6-di-O-benzyl-β-D-glucopyranoside 62867-63-4 C29H33NO6
benzyl 2-acetamido-2-deoxy-3,6-di-O-benzyl-β-D-glucopyranoside
—— 1α,3β-bis<(tert-butyldimethylsilyl)oxy>-23,24-bisnorchol-5,7-dien-22-ol 126771-88-8 C34H62O3Si2
1α,3β-bis<(tert-butyldimethylsilyl)oxy>-23,24-bisnorchol-5,7-dien-22-ol
—— 1α,3β-bis[(tert-butyldimethylsilyl)oxy]-5α,8α-(3,5-dioxo-4-phenyl-1,2,4-triazolidine-1,2-diyl)-23,24-bisnorchol-6-en-22-ol 174201-34-4 C42H67N3O5Si2
1α,3β-bis[(tert-butyldimethylsilyl)oxy]-5α,8α-(3,5-dioxo-4-phenyl-1,2,4-triazolidine-1,2-diyl)-23,24-bisnorchol-6-en-22-ol
—— 2,5-bis(2-(2-methoxyethoxy)ethoxy)terephthalaldehyde 1628897-24-4 C18H26O8
2,5-bis(2-(2-methoxyethoxy)ethoxy)terephthalaldehyde
—— 7-(2-Bromo-acetylamino)-3-methyl-8-oxo-5-thia-1-aza-bicyclo[4.2.0]oct-2-ene-2-carboxylic acid 58197-02-7 C10H11BrN2O4S
7-(2-Bromo-acetylamino)-3-methyl-8-oxo-5-thia-1-aza-bicyclo[4.2.0]oct-2-ene-2-carboxylic acid
—— 1-methoxy-3,5-diamino-benzene 100-96-9 C7H10N2O
1-methoxy-3,5-diamino-benzene
—— 2-hydroxy-2-methyl-2-(4'-methylphenyl)acetonitrile 69813-74-7 C10H11NO
2-hydroxy-2-methyl-2-(4'-methylphenyl)acetonitrile
—— 1,3,5-tris(methoxymethyl)benzene 84941-01-5 C12H18O3
1,3,5-tris(methoxymethyl)benzene
—— 5’-O-DMT-N2-isobutyrylguanosine 81246-83-5 C35H37N5O8
5’-O-DMT-N2-isobutyrylguanosine
—— 2-(pyrimidin-4-yl)nicotinic acid 1429555-05-4 C10H7N3O2
2-(pyrimidin-4-yl)nicotinic acid
—— (2R)-1,4-dioxan-2-yl-N-methylmethanaminium chloride 917882-58-7 C6H13NO2*ClH
(2R)-1,4-dioxan-2-yl-N-methylmethanaminium chloride
—— 6-(7-methoxyquinolin-4-yloxy)-1-naphthoic acid 847803-42-3 C21H15NO4
6-(7-methoxyquinolin-4-yloxy)-1-naphthoic acid
—— biphenyl-2-yl-carbamic acid 1-[2-(benzylmethylamino)ethyl]piperidin-4-yl ester 864686-28-2 C28H33N3O2
biphenyl-2-yl-carbamic acid 1-[2-(benzylmethylamino)ethyl]piperidin-4-yl ester
—— 4,4'-biphenyldiol bis[di(2,6-dimethylphenyl)phosphate] 147263-99-8 C44H44O8P2
4,4'-biphenyldiol bis[di(2,6-dimethylphenyl)phosphate]
—— benzyl N-(2,2-dimethoxyethyl)-N-methyl-carbamate 1355573-66-8 C13H19NO4
benzyl N-(2,2-dimethoxyethyl)-N-methyl-carbamate
—— 1-((3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)sulfonyl)pyrrolidine 1509932-05-1 C16H24BNO4S
1-((3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)sulfonyl)pyrrolidine
—— 2,3,5-trimethylcyclohexanol 116-02-9 C9H18O
2,3,5-trimethylcyclohexanol
—— 2-(3-bromophenyl)dibenzofuran 1084334-27-9 C18H11BrO
2-(3-bromophenyl)dibenzofuran
—— 6-methyl-2-(phenylmethoxy)benzoic acid 118537-95-4 C15H14O3
6-methyl-2-(phenylmethoxy)benzoic acid
—— 3-(4-chlorophenyl)-3-oxopropanoic acid 17589-68-3 C9H7ClO3
3-(4-chlorophenyl)-3-oxopropanoic acid
—— 1,4-bis((oxiran-2-ylmethoxy)methyl)benzene 29513-13-1 C14H18O4
1,4-bis((oxiran-2-ylmethoxy)methyl)benzene
—— 5-Dehydro-shikimisaeure 2922-42-1 C7H8O5
5-Dehydro-shikimisaeure
—— trans-1,2-Diamino-cyclohexan-N,N.N',N'-tetraessigsaeure 13291-61-7 C14H22N2O8
trans-1,2-Diamino-cyclohexan-N,N.N',N'-tetraessigsaeure
—— 4'-bromo-2,6-dimethoxy-1,1'-biphenyl 168849-77-2 C14H13BrO2
4'-bromo-2,6-dimethoxy-1,1'-biphenyl
—— 9-(4-methylphenyl)fluorene 18153-43-0 C20H16
9-(4-methylphenyl)fluorene
—— (E)-2-hydroxy-N’-((2-hydroxynaphthalen-1-yl)methylene)benzohydrazide 1099592-35-4 C18H14N2O3
(E)-2-hydroxy-N’-((2-hydroxynaphthalen-1-yl)methylene)benzohydrazide