Intermediates
Intermediates are chemical compounds formed during the various stages of active pharmaceutical ingredient (API) production. They are essentially the “building blocks” in the multi-step synthesis process that eventually leads to the final API. Intermediates are not the finished product but play a crucial role in ensuring the successful creation of high-quality APIs.
These intermediates can be classified as key starting materials (KSMs) or other intermediates, depending on where they fall within the synthesis process. The production and handling of intermediates are subject to stringent regulations to ensure they meet purity and quality requirements, as any impurities could carry over to the final API.
Intermediates are also an important part of the global pharmaceutical supply chain. Many intermediates are manufactured by specialized companies and then sold to API producers, fostering collaboration within the industry. The complexity of these intermediates can vary significantly, depending on the sophistication of the API being synthesized.
| API | Intermediate Name | CAS No. |
|---|---|---|
| Fluconazole | 1-(2,4-Diflurophenyl)-1-(1H-1,2,4-triazole-1yl)-ethanone (DFTA) | 873055-58-4 |
| Voriconazole | (2R, 3S/2S, 3R)-3-(5-Fluoropyrimidin-4-yl)-2-(2,4-di-fluorophenyl)-1-(1H-1,2,4 triazol-1-yl) butan-2-ol {Racemic Voriconazole} | 873055-58-4 |
| (2R, 3S)-2-(2,4-Difluorophenyl)-3-(5-fluoropyrimidine-4yl)-1-(1H-1,2,4 triazol-1-yl) butan-2-ol {camphor sulfonate | 1327234-71-0 | |
| Posaconazole | (S)-(+)-4Phenyl-2-oxazolidinone | 99395-88-7 |
| (R)-(-)-4-Phenyl-2-oxazolidinone | 90319-52-1 | |
| Efavirenz | Cyclopropyl Acetylene | 6746-94-7 |
| Cyclopropyl Methyl Ketone | 765-43-5 | |
| Valganciclovir Hcl | N-2-Acetylguanine | 19962-37-9 |
| CBZ-valganciclovir | 194154-40-0 | |
| Mono-o-acetate Ganciclovir | 88110-89-8 | |
| Triacetylganciclovir | 86357-14-4 | |
| 1,3-Dichloro-2-(acetoxymethoxy)propane | 89281-73-2 | |
| 1,3-Diacetoxy-2-(acetoxymethoxy)propane | 86357-13-3 | |
| Vildagliptin | (2S)-1-(Chloroacetyl)-2-pyrrolidinecarbonitrile | 207557-35-5 |
| L-Prolinamide | 7531-52-4 | |
| 3-Amino-1-hydroxyadamantane | 702-82-9 | |
| 1-Adamantanamine hydrochloride | 665-66-7 | |
| 3-amino-1-adamantanol | 702-82-9 | |
| Linagliptin | (R)-3-(Boc-Amino)piperidine | 309956-78-3 |
| N-Boc Linagliptin | 668273-75-4 | |
| 8-Bromo-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydro-purine-2,6-dione | 853029-57-9 | |
| 2-(Cloromethyl)-4-methylquinazoline | 109113-72-6 | |
| 8-Bromo-7-(but-2-yn-1-yl)-3-methyl-1H-purine-2,6(3H,7H)-dione | 666816-98-4 | |
| Imeglimin Hydrochloride | Imeglimin base | 775351-65-0 |
| N2,N2,6-trimethyl-1,6-dihydro-1,3,5-triazine-2,4-diamine | 757178-57-7 | |
| 1,3,5-Triazine-2,4-diamine,3,6-dihydro-N2,N2,6-trimethyl-, (6R)-, (2R,3R)-2,3-dihydroxybutanedioate | 1016979-78-4 | |
| Sitagliptin Phosphate | Tert-butyl N-[(2R)-4-oxo-4-[3-(trifluoromethyl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-1-(2,4,5-trifluorophenyl)butan-2-yl]carbamate | 486460-23-5 |
| 3-(Trifluoromethyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine hydrochloride | 762240-92-6 | |
| Boc-(R)-3-Amino-4-(2,4,5-trifluorophenyl)butanoic acid | 486460-00-8 | |
| (3R)-3-Amino-1-[3-(trifluoromethyl)-5,6,7,8-tetrahydro-1,2,4-triazolo[4,3-a]pyrazin-7-yl]-4-(2,4,5-trifluorophenyl)butan-1-one | 486460-32-6 | |
| Dapagliflozin | (3R,4S,5R,6R)-3,4,5-tris(triMethylsilyloxy)-6-((triMethylsilyloxy)Methyl)tetrahydro-2H-pyran-2-one | 32384-65-9 |
| (2R,3R,4R,5S,6S)-2-(Acetoxymethyl)-6-(4-chloro-3-(4-ethoxybenzyl)phenyl)tetrahydro-2H-pyran-3,4,5-triyl triacetate | 461432-25-7 | |
| Losartan Potassium | (1-((2'-(1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-2-butyl-4-chloro-1H-imidazol-5-yl)methanol | 114798-26-4 |
| Nirmatrelvir | Methyl(S)-2-((tert-butoxycarbonyl)amino)-3-((S)-2-oxopyrrolidin-3-yl)propanote (SM1) | 328086-60-8 |
| 3-Pyrrolidinepropanamide,α-amino-2-oxo-,hydrochloride (T13) | 2628280-48-6 | |
| (1R,2S,5S)-6,6-dimethyl-3-aza-bicylo[3.1.0]hexane-2-carboxylic acid methyl ester hydrochloride (SM2) | 565456-77-1 | |
| Rivaroxaban | 2-[(2R)-2-hydroxy-3-[[4-(3-oxomorpholin-4-yl)phenyl]amino]propyl]-1H-isoindole-1,3(2H)-dione | 446292-07-5 |
| 2-([(5S)-2-oxo-3-[4-(3-oxomorpholin-4-yl)phenyl]-1,3-oxazolidin-5-yl]methyl)-1H-isoindole-1,3(2H)-dione | 446292-08-6 | |
| 4-[4-[(5S)-5-(Aminomethyl)-2-oxo-3-oxazolidinyl]phenyl]-3-morpholinone hydrochloride | 898543-06-1 | |
| Tapendatol HCl | (S)-3-(dimethylamino)-1-(3-methoxyphenyl)-2-methylpropan-1-one | 850222-40-1 |
| (2S,3R)-1-(Dimethylamino)-3-(3-methoxyphenyl)-2-methylpentan-3-ol | 809282-20-0 | |
| (betaR,gammaR)-gamma-Ethyl-3-methoxy-N,N,beta-trimethylbenzenepropanamine | 175591-22-7 | |
| 2R,3R)-1-(DiMethylaMino)-3-(3-Methoxyphenyl)-2-Methylpentan-3-ol hydrochloride | 175590-75-7 | |
| Lamivudine | (1R,2S,5R)-Menthyl-(2R,5S)-5-(4-amino-2-oxo-2H-pyrimidin-1-yl)-[1,3 oxathiolene-2-carboxylic acid | 147027-10-9 |
| 92R-cis)hidroxybenzoate-4-amino-1-[(2-hidroxy-methyl)-1,3-oxat iolan-5-il]-2-(1H)-pirimidinone | 173522-96-8 | |
| Emtricitabine | (2R,5S)-5-(4-Amino-5-fluoro-2-oxo-1(2H)-pyrimidinyl)-1,3-oxathiolane-2-carboxylic acid,(1R,2S,5R)-5-methyl-2-(1-methylethyl)cyclohexyl ester | 764659-72-5 |
| Darunavir/ Darunavir Ethanolate | 4-Amino-N-((2R,3S)-3-amino-2-hydroxy-4-phenylbutyl)-N-isobutylbenzenesulfonamide | 169280-56-2 |
| (3aS,4S,6aR)-4-methoxy-tetrahydro-furo[3,4-b]furan-2(3H)-one | 866594-60-7 | |
| [(3R,3aS,6aR)-Hydroxyhexahydrofuro[2,3-b]furanyl Succinimidyl Carbonate | 253265-97-3 | |
| Ritonavir | 1-(2-isopropylthiazol-4-yl)-N-methylmethanamine dihydrochloride | 1185167-55-8 |
| [(S)-2-(3-((2-isopropylthiazol-4-yl)methyl)-3-methylureido)-3-methylbutanoic acid] | 154212-61-0 | |
| [4-nitrophenyl thiazol-5-ylmethyl carbonate] | 144163-97-3 | |
| Lopinavir | 2-(2,6-dimethylphenoxy)acetic acid | 13335-71-2 |
| (S)-3-methyl-2-(2-oxotetrahydropyrimidin-1(2H)-yl-butanoic acid | 192725-50-1 | |
| Raltegravir Potassium | [1-[4-[[(4-fluorobenzyl)amino]carbonyl]-5-hydroxy-1-methyl-6-oxo-1,6-dihydropyrimidin-2-yl]-1-methylethyl]carbamate) | 518048-02-7 |
| 5-Methyl-1,3,4-oxadiazole-2-carboxylic acid potassium salt | 888504-28-7 | |
| Abacavir Sulfate | (1R,4S)-4-amino-2-cyclopentene-1-methanol hydrchloride | 287717-44-6 |
| 2-amino-4,6-dichloro-5-formamidopyrimidine | 171887-03-9 | |
| Rilpivirine Hcl | 4-[(4-hydroxy-2-pyrimidinyl)amino]benzonitrilr | 189956-45-4 |
| 4[(4-Chloro-2-pyrimidinyl)amino]nenzonitrile | 244768-32-9 | |
| 4-Iodo-2,6-dimethylaniline | 4102-53-8 | |
| 3-(4-amino-3,5-dimethylphenylprop-2-enamide | 500292-92-2 | |
| (E)-3-(4-Amino-3,5-dimethylphenyl)-2-propenenitrile hydrchloride | 661489-23-2 | |
| Tigecycline | N-tert-Butylglycine HCl | 6939-23-7 |
| 9-Amino Minocycline HCl | 149934-21-4 | |
| 9-Amino Minocycline Sulfate | 149934-20-3 | |
| Minoxidil | 4-Chloro-2,6-diaminopyramidine | 156-83-2 |
| Oxcarbazepine | 10-Methoxyiminostilbene | 4698-11-7* |
| Isavuconazole | (2R,3R)-3-(2,5-Difluorophenyl)-3-hydroxy-2-Methyl-4-(1H-1,2,4-triazol-1-yl)thiobutyramide | 368421-58-3 |
| 4-(2-bromoacetyl)benzonitrile | 20099-89-2 | |
| Glycine, N-[(1,1-dimethylethoxy)carbonyl]-Nmethyl-[2-[[(1-cholroethoxy)carbonyl]Methylamino]-3-pyridinyl]methylester | 338990-31-1 | |
| Tirzepatide | AEEA-AEEA | 1143516-05-5 |
| Fmoc-L-Lys[C20-OtBu-Glu(OtBu)-AEEA-AEEA]OH | 2915356-76-0 | |
| Ly1001 | 1188328-37-1 | |
| N-(9-Fluorenylmethoxycarbonyl)-L-alanine | 207291-76-7 | |
| Fmoc-L-Lys(Dde)-OH | 150629-67-7 | |
| Fmoc-his(Trt)-OH | 109425-51-6 | |
| Fmoc-D-Trp(Boc)-OH | 163619-04-3 | |
| Retatrutide | Fmoc-L-Lys-[C20-OtBu-Glu(OtBu)-AEEA]-OH | 2612237-97-3 |
| AZD-5305 | 2589531-76-8 | |
| 2-Pyridincarboxamide,N-methyl-5-(1-piperazinyl)- | 2259835-10-2 | |
| 2-Trifluoromethyl Thioxanthone | 1693-28-3 | |
| Triethylamine | 121-44-8 | |
| 4-Bromo-2-fluorobenzoic acid | 112704-79-7 | |
| Methyl(S)-2-(Boc-amino)-3-[(S)-2-oxo-3-pyrrolidinyl]propanoate | 328086-60-8 | |
| 2,3-Dihydroxypyridine | 16867-04-2 | |
| 2-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)acetonitrile | 68119-31-3 | |
| 1-(2,2-Difluoro-benzo[1,3]dioxol-5-yl)-cyclopropanecarboxylicacid | 862574-88-7 | |
| DMF-DMA | 4637-24-5 | |
| Favipiravir | 2-pyrazinecarboxamide,3,4-dihydro-3-oxo-sodium salt (1:1) | 1237524-82-1 |
| Bedaquiline Fumarate | N-(4-Bromo-phenyl)-3-phenyl-propionamide | 316146-27-7 |
| 3-benzyl-6-bromo-2-chloroquinoline | 654655-68-2 | |
| 3-benzyl-6-bromo-2-methoxyquinoline | 654655-69-3 | |
| 3-(dimethylamino)-1-(napthalene-1-yl)propan-1-one hydrochloride | 5409-58-5 |