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:
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。
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。
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。
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。
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。
中文名称 | 英文名称 | CAS号 | 化学式 | 结构式图片 |
---|---|---|---|---|
(R)-6-(4-氨基苯基)-4,5-二氢-5-甲基-3(2H)-哒嗪酮 | (R)-6-(4-aminophenyl)-5-methyl-4,5-dihydropyridazin-3(2H)-one | 101328-85-2 | C11H13N3O |
|
(R)-5-[2-[(5,6-二乙基-2,3-二氢-1H-茚-2-基)氨基]-1-羟基乙基]-8-(苄氧基)-2(1H)-喹啉酮 | 8-(phenylmethoxy)-5-[(R)-2-(5,6-diethyl-indan-2-ylamino)-1-hydroxy-ethyl]-(1H)-quinolin-2-one | 435273-75-9 | C31H34N2O3 |
|
(R)-5-(2-(2,5-二氟苯基)吡咯烷-1-基)-3-硝基吡唑并[1,5-A]嘧啶 | (R)-5-(2-(2,5-difluorophenyl)pyrrolidin-1-yl)-3-nitropyrazolo[1,5-a]pyrimidine | 1223404-90-7 | C16H13F2N5O2 |
|
(R)-4-羟基-N,N-二苯基-2-戊炔酰胺 | (R)-4-hydroxy-N,N-diphenylpent-2-ynamide | 899809-61-1 | C17H15NO2 |
|
(R)-3-苯基哌啶 | (R)-3-phenylpiperidine | 430461-56-6 | C11H15N |
|
(R)-3-羟基吡咯烷盐酸盐 | (R)-3-hydroxypyrrolidine hydrochloride | 104706-47-0 | C4H9NO*ClH |
|
(R)-3-氨基-4-(2,4,5-三氟苯基)丁酸 | (R)-3-amino-4-(2,4,5-trifluorophenyl)butyric acid | 936630-57-8 | C10H10F3NO2 |
|
(R)-3-Boc-氨基哌啶 | (R)-piperidin-3-ylcarbamic acid tert-butyl ester | 309956-78-3 | C10H20N2O2 |
|
(R)-3-(甲基氨基)-1-苯基-1-丙醇 | (R)-N-methyl-3-phenyl-3-hydroxypropylamine | 115290-81-8 | C10H15NO |
|
(R)-3-(Boc-氨基)-2-苯丙酸 | (R)-3-(Boc-amino)-2-phenylpropionic acid | 181140-88-5 | C14H19NO4 |
|
(R)-3,3′-双(三苯甲硅烷基)-1,1′-联-2-萘酚 | (R)-1-(2-hydroxy-3-(triphenylsilyl)naphthalen-1-yl)-3-(triphenylsilyl)naphthalen-2-ol | 111822-69-6 | C56H42O2Si2 |
|
(R)-3,3-二甲基-2-丁胺 | (R)-1,2,2-trimethylpropylamine | 66228-31-7 | C6H15N |
|
(R)-2-苄氧基-1-丙醇 | (R)-2-(benzyloxy)propan-1-ol | 87037-69-2 | C10H14O2 |
|
(R)-2-氧代四氢呋喃-3-基氨基甲酸苄酯 | (+)-D-N-benzyloxycarbonylhomoserinolactone | 41088-89-5 | C12H13NO4 |
|
(R)-2-氧代四氢呋喃-3-基氨基甲酸叔丁酯 | (R)-2-[(tert-butoxycarbonyl)amino]butano-4-lactone | 67198-86-1 | C9H15NO4 |
|
(R)-2-(2-氯苯基)吡咯烷 | (R)-2-(2-chlorophenyl)pyrrolidine | 823188-58-5 | C10H12ClN |
|
(R)-2-((S)-2,2-二-5-OXO-1,3-二氧戊环-4-YL)-3-(萘-2-基)丙酸 | (R)-2-((S)-2,2-dimethyl-5-oxo-1,3-dioxolan-4-yl)-3-(naphthalen-2-yl)propanoic acid | 198568-07-9 | C18H18O5 |
|
(R)-2,5-二氢-3,6-二乙氧基-2-异丙基吡嗪 | (2R)-3,6-diethoxy-2-isopropyl-2,5-dihydropyrazine | 110117-71-0 | C11H20N2O2 |
|
(R)-2,4-二氯-ALPHA-甲基-苯甲胺 | (R)-2,4-dichloro-α-methylbenzylamine | 133773-29-2 | C8H9Cl2N |
|
(R)-1-氨基丙烷-2-氨基甲酸苄酯 | (R)-benzyl 1-aminopropan-2-ylcarbamate | 346669-50-9 | C11H16N2O2 |
|
(R)-1-叔丁氧羰基-2-乙基哌嗪 | tert-butyl (R)-2-ethylpiperazine-1-carboxylate | 393781-70-9 | C11H22N2O2 |
|
(R)-1-N-叔丁氧羰基哌嗪-3-甲酸甲酯 | 1-(tert-butyl) 3-methyl (R)-piperazine-1,3-dicarboxylate | 438631-77-7 | C11H20N2O4 |
|
(R)-1-Boc-3-羟基哌啶 | tert-butyl (3R)-3-hydroxypiperidine-1-carboxylate | 143900-43-0 | C10H19NO3 |
|
(R)-1-Boc-3-羟基吡咯烷 | (R)-N-tert-butyloxycarbonyl-3-pyrrolidinol | 109431-87-0 | C9H17NO3 |
|
(R)-1-(甲氧基(甲基)氨基)-1-氧代-2-丙基氨基甲酸叔丁酯 | tert-butyl N-[(1R)-2-[methoxy(methyl)amino]-1-methyl-2-oxo-ethyl]carbamate | 146553-06-2 | C10H20N2O4 |
|
(R)-1-(3-氯苯基)乙醇 | (R)-1-(3-chlorophenyl)-ethanol | 120121-01-9 | C8H9ClO |
|
(R)-1-(3-氯苯基)乙胺 | (R)-1-(3-chlorophenyl)ethanamine | 17061-53-9 | C8H10ClN |
|
(R)-1-(2-氟苯基)乙胺 | (R)-1-(2-fluorophenyl)ethan-1-amine | 185545-90-8 | C8H10FN |
|
(R)-1-(2,6-二氯-3-氟苯基)乙醇 | (R)-1-(2,6-dichloro-3-fluorophenyl)ethanol | 330156-50-8 | C8H7Cl2FO |
|
(R)-1,2-二噻茂烷-3-戊酸钠 | sodium lipoic acid | 176110-81-9 | C8H13O2S2*Na |
|
(R)-(-)-8a-甲基-3,4,8,8a-四氢-1,6(2H,7H)-萘二酮 | (R)-Wieland-Miescher ketone | 100348-93-4 | C11H14O2 |
|
(R)-(-)-3-氨基哌啶 二盐酸盐 | (R)-3-Aminopiperidine dihydrochloride | 334618-23-4 | C5H14Cl2N2 |
|
(R)-(-)-3-(氨甲酰甲基)-5-甲基己酸 | (R)-(-)-3-(carbamoylmethyl)-5-methylhexanoic acid | 181289-33-8 | C9H17NO3 |
|
(R)-(-)-2-甲基戊二酸 | (R)-2-methylglutaric acid | 1115-81-7 | C6H10O4 |
|
(R)-(-)-1-氨基茚盐酸盐 | (R)-2,3-dihydro-1H-inden-1-amine hydrochloride | 10305-73-4 | C9H11N*ClH |
|
(R)-(+)-叔丁基亚磺酰胺 | (R)-2-methylpropane-2-sulfinamide | 196929-78-9 | C4H11NOS |
|
(R)-(+)-alpha-氨基-gamma-丁内酯盐酸盐 | (R)-α-amino-γ-butyrolactone hydrochloride | 104347-13-9 | C4H7NO2*ClH |
|
(R)-(+)-5’-甲氧基劳丹素 | 5'-methoxylaudanosine | 24734-71-2 | C22H29NO5 |
|
(R)-(+)-3-羟基-3-苯丙酸 | (R)-3-phenyl-3-hydroxypropionic acid | 2768-42-5 | C9H10O3 |
|
(R)-(+)-2-苄氧基丙酸 | (R)-2-benzyloxypropionic acid | 100836-85-9 | C10H12O3 |
|
(E)-辛-4-烯-1,8-二酸 | (E)-oct-4-ene-1,8-dioic acid | 48059-97-8 | C8H12O4 |
|
(E)-乙苯亚甲基丁二酸 | trans-phenylitaconic acid | 5653-88-3 | C11H10O4 |
|
(E)-beta-(4-氯苯基)丙烯酰苯 | 4-chlorochalcone | 22252-16-0 | C15H11ClO |
|
(E)-N-(2-氯-6-甲基苯基)-3-乙氧基丙烯酰胺 | (E)-N-(2-chloro-6-methylphenyl)-3-ethoxyacrylamide | 863127-76-8 | C12H14ClNO2 |
|
(E)-3-[2-(7-氯-2-喹啉基)乙烯基]苯甲醛 | (E)-3-[2-(7-chloro-2-quinolinyl)ethenyl]benzaldehyde | 120578-03-2 | C18H12ClNO |
|
(E)-3-(5-硝基-1-环己烯-1-基)丙烯酸 | 3-(5-nitro-cyclohex-1-enyl)-acrylic acid | 899809-64-4 | C9H11NO4 |
|
(E)-3-(3,4-二甲氧基苯基)-1-(3-羟基苯基)-1-丙酮 | (E)-3-(3,4-dimethoxyphenyl)-1-(3-hydroxyphenyl)prop-2-en-1-one | 178445-80-2 | C17H16O4 |
|
(E)-3,4,5-三甲氧基苯甲醛肟 | (E)-3,4,5-trimethoxybenzaldehyde oxime | 39201-89-3 | C10H13NO4 |
|
(E)-2-甲基-2-丁烯酸异丙酯 | disodium;3-[[4-[(3-carboxy-4-oxidophenyl)diazenyl]benzoyl]amino]propanoate | 213594-60-6 | C17H13N3Na2O6 |
|
(E)-2-[2-(6-氯嘧啶-4-基氧)苯基]-3-甲氧基丙烯酸甲酯 | (E)-methyl 2-(2-((6-chloropyrimidin-4-yl)oxy)-phenyl)-3-methoxyacrylate | 131860-97-4 | C15H13ClN2O4 |
|