In cell biology, intermediate refers to the middle part of spindle which gradually disintegrates near the equatorial plane in the late stage of cell division, and the concentration of cytoplasm around it increases, filling the whole equatorial plane. This dense area is called the middle area. 2-Chloro-3-Bromo Pyridine
2- chloro -5- bromopyridine
3- bromo -5- cyanopyridine
3- bromo -5- chloropyridine
2- amino -5- methylpyridine
Phenylboronic acid series:
3,4-dichlorophenylboronic acid
3,5-dichlorophenylboronic acid
3,4,5-trichlorophenylboronic acid
2,4,6-trichlorophenylboronic acid
2,6-dimethylphenylboronic acid
3,5-dimethylphenylboronic acid
2- chlorophenylboronic acid
3- hydroxymethyl phenylboronic acid
Iodopyridine series:
2- chloro -3- iodopyridine
2- fluoro -3- iodopyridine
2- amino -3- iodopyridine
5- iodouracil
2,4-dichloro -5- iodopyrimidine
5- bromopyridine -2- carboxylic acid
2- formyl -5- hydroxypyridine
2- acetyl -5- hydroxypyridine
2- fluoro -4- iodopyridine
2- iodo -5- hydroxypyridine
2- iodo -3- hydroxypyridine
2- amino -3- iodopyridine
2- chloro -3- aminopyridine
2- chloro -4- aminopyridine
4- bromopyridine hydrochloride 1)
After nearly 50 years of development, β -lactam antibiotics have formed a complete production system. Almost all β -lactam antibiotics (except those within the patent period) can be produced at low cost in China. The output of penicillin ranks first in the world and is exported to the international market in large quantities. Cephalosporins are basically self-sufficient and some of them can be exported.
Intermediates matching with β -lactam antibiotics can be produced domestically, and side chain intermediates can be produced and exported in large quantities, except for semi-synthetic antibiotic mother nuclei 7-ACA and 7-ADCA, which need to be partially imported.
Take phenylacetic acid as an example, the main supporting intermediate of β -lactam antibiotics. There are nearly 30 phenylacetic acid production enterprises in China, with an annual total production capacity of about 20,000 tons. But most enterprises are small in scale, with the largest annual output of 2,000 tons, and most others have an annual output of several hundred tons. In 2003, the domestic total demand of phenylacetic acid was about 6.5438+0.4 million tons, and the consumption structure was: penicillin G accounted for 85%, other drugs accounted for 4%, spices accounted for 7%, and pesticides and other fields accounted for 4%.
With the development of domestic perfume, medicine, pesticide and other industries, the demand for phenylacetic acid will further increase. It is estimated that by 2005, China's pharmaceutical industry will consume about 1.4 million tons of phenylacetic acid, 500 tons of pesticide industry and 2000 tons of perfume industry. Together with consumption in other fields, it is estimated that the total domestic demand of phenylacetic acid will reach 654.38+800,000 tons in 2005.
2) notch
China has become the largest producer of antipyretic and analgesic drugs in the world, with the output of aspirin, paracetamol and metamizole all exceeding 1 10,000 tons, and the output of phenacetin, aminopyrine and antipyrine exceeding 654.38+10,000 tons. At present, the output of antipyretic and analgesic drugs in China is growing rapidly, and it is expected to increase at a rate of about 8% in the future. The production of antipyretic and analgesic intermediates is large and there are many manufacturers. With the growth of antipyretic and analgesic drugs, intermediates have also developed greatly.
In 2003, the consumption of acetaminophen in China increased rapidly, and the export also showed a rapid growth momentum. The export volume is 28 163 tons, and the annual export volume increases by about 1 times. By the first half of 2004, although the export growth rate slowed down, it still increased. From June 5438 to May 2004, the export volume of paracetamol was 1250 1 ton, slightly higher than the same period last year. P-aminophenol is an important intermediate for the synthesis of paracetamol, which is developing rapidly. The annual output of p-aminophenol in China is about 32,000 tons. It is predicted that by 2005, the domestic production of acetaminophen will reach more than 50,000 tons, and the pharmaceutical industry will consume 45,000 tons of acetaminophen. Combined with its application in other fields, the total demand of p-aminophenol in 2005 was about 50,000 tons, with a large market gap and broad prospects for development and utilization. The demand for phenylacetic acid will continue to grow. Up to 20 12, the quinolones developed and put into mass production in China mainly include norfloxacin, ciprofloxacin, ofloxacin, enoxacin, lomefloxacin and fleroxacin. Among them, norfloxacin, ciprofloxacin and ofloxacin have the largest output, accounting for about 98% of the total fluoroquinolones in China.
Quinolones are generally fluoroquinolones synthesized by fluorobenzene ring, and then condensed with piperazine (or methylpiperazine). Due to the abundant fluorite reserves in China, it is one of the countries with the largest output of fluorine-containing drugs and intermediates in the world, and more than 80% of fluorine-containing intermediates are exported. On the whole, China's fluorobenzene intermediates developed earlier and the production capacity was generally surplus; The intermediate of trifluorotoluene developed late and quickly; For heterocyclic aromatic compounds, especially fluoropyridine, only a few research units and manufacturers in China have the synthesis technology of fluoropyridine intermediates. Therefore, the fluoropyridine intermediate will become one of the main directions of domestic fluorine intermediate research and development in the next few years. Intermediate of entecavir: step 1:
3- cyclopentene-1- alcohol, 2- thiadiazole thiadiazole thiadiazole thiadiazole thiadiazole thiadiazole [3, racecadotril racecadotril 2-a] quinoline -3- carboxylic acid racecadotril racecadotril racecadotril racecadotril intermediate: 3- acetyl thio-.
6- fluoro -3- (tetrahydropyrrolidine -4- yl) benzo [b] isoxazole 6- fluoro -3-(4- piperidinyl)-1, 2- benzoisoxazole
3-(2- chloroethyl) -2- methyl-6,7,8,9-tetrahydro-pyrido [1, 2-a] pyrimidine -4- one 3-(2- chloroethyl)-6,7,8,9-tetrahydro.
5-{ 4-{ 2-[ methyl -(2- pyridyl) amino] ethoxy} benzyl}-2,4- thiazole-dione 5-{ 4-{ 2-[ methyl -(2- pyridyl) amino] ethoxy} benzyl}-2,4.
Roxitin acetate hydrochloride Roxitin acetate hydrochloride intermediate: 3-( 1- piperidylmethyl) phenol 3-( 1- piperidylmethyl) phenol.
N-{ 3-[3-( 1- piperidylmethyl) phenoxy] propyl} amine n-{ 3-[3-( 1- piperidylmethyl) phenoxy]} propylamine telmisartan intermediate:
N- methyl-o-phenylenediamine dihydrochloride
2- n-propyl -4- methyl -6- carboxybenzimidazole 2- propyl -4- methyl -6- carboxybenzimidazole
4 '- methyl diphenyl -2- carboxylic acid tert-butyl ester 4 '- methyl biphenyl -2- carboxylic acid tert-butyl ester
4'- (bromomethyl) biphenyl -2- tert-butyl carboxylate 4 '- bromomethyl biphenyl -2- tert-butyl formate
Intermediate of trospium chloride trospium chloride: α-hydroxy-α-phenylphenylacetic acid.
Voriconazole Voriconazole Intermediate:
6-( 1- bromo-ethyl) -4- chloro -5- fluoropyrimidine
1-(2,4-difluorophenyl) -2-( 1H- 1, 2,4-triazole-1- yl)-1- ethyl ketone1-
(2R, 3S/2S, 3R)-3-(4- chloro -5- fluoro -6- pyrimidinyl) -2- (2,4- difluorophenyl)-1-( 1H- 1, 2,4-)
(2R, 3S/2S, 3R)-3-(4- chloro -5- fluoropyrimidine -6- yl)-2-(2,4- difluorophenyl)-1- (1h- 1, 2,4-) 4- difluorophenyl)-1-( 1H- 1, 2,4-triazole-1- yl) -2- butanol
(2r, 3s/2s, 3r)-3-(5- fluoropyrimidine -4- yl)-2-(2,4- difluorophenyl)-1-( 1h- 1, 2,4-triazole-6544.
Ziprasidone Ziprasidone Intermediate:
3-( 1- piperazinyl)-1, 2- benzisothiazole hydrochloride 3-( 1- piperazinyl)-1, 2- benzisothiazole hydrochloride zolmitriptan zolmitriptan/zolmitriptan intermediate: (s)-4.
Imatinib mesylate and its intermediate imatinib mesylate base
4-[(4- methyl-1- piperazinyl) methyl] benzoic acid
4-[(4- methyl-1- piperazinyl) methyl] benzoic acid dihydrochloride N-(5- amino -2- methylphenyl) -4-(3- pyridyl) -2- pyrimidine-amine
Sunitinib and its intermediate sunitinib base
5- fluoro-1, 3- dihydroindole -2- one
2- tert-butyl 4- ethyl 3,5-dimethyl-1H- pyrrole -2,4- dicarboxylate 4-(ethoxycarbonyl)-3,5-dimethyl-1H- pyrrole -2- carboxylate 2,4-dimethyl-/kloc-0.
5-((Z)-(5- fluoro -2- oxoindoline -3- subunit) methyl) -2,4-dimethyl-1H- pyrrole -3- carboxylic acid
Rapatinib and its Intermediate Rapatinib Base
2- amino -5- iodo-benzoic acid 6- iodoquinazolone 4- chloro -6- iodoquinazoline
2- chloro-1-(3- fluoro-benzyloxy) -4- nitrobenzene 3- chloro -4-(3- fluoro-benzyloxy)-aniline
N-{ 3- chloro -4-[(3- fluorobenzyl) oxy] phenyl }-6- iodoquinazoline -4- amine 5-[4-({ 3- chloro -4-[(3- fluorobenzyl) oxy] phenyl} amino) quinazoline -6- yl]-2
Nilotinib and its intermediate Nilotinib
4- methyl -3-[[4-(3- pyridyl) -2- pyrimidinyl] amino] benzoic acid 4- methyl -3-[[4-(3- pyridyl) -2- pyrimidinyl] amino] ethyl benzoate.
3-[ (aminoiminomethyl) amino]-p-toluic acid ethyl mononitrate 3-(4- methyl-1H- imidazole-1- yl) -5- (trifluoromethyl) aniline.
Dasatinib and its intermediate Dasatinib
2- amino -N-(2- chloro -6- methylphenyl) thiazole -5- carboxamide
2-(6- chloro -2- methylpyrimidine -4- ylamino) -N-(2- chloro -6- methylphenyl) thiazole -5- carboxamide
Gefitinib and its intermediate Gefitinib
Methyl 2- amino -4,5-dimethoxybenzoate 6,7- dimethoxyquinazolin -4(3H)- ketone 6- hydroxy -7- methoxyquinazolin -4(3H)- ketone
3,4- dihydro -7- methoxy -4- oxoquinazoline -6- yl acetate 4- chloro -7- methoxyquinazoline -6- yl acetate
4-(3- chloro -4- fluorophenyl amino) -7- methoxyquinazoline -6- yl acetate (HCl)
4-(3- chloro -4- fluorophenyl amino) -7- methoxyquinazoline -6- ol 4-(3- chloropropyl) morpholine
Erlotinib and its intermediates
Erotinib/ erlotinib base
Ethyl 3,4-dihydroxy benzoate
3,4-bis (2- methoxyethoxy) ethyl benzoate 4,5-bis (2- methoxyethoxy) -2- ethyl nitrobenzoate 4,5-bis (2- methoxyethoxy) -2- ethyl aminobenzoate 6,7-bis -(2- methoxyethoxy)-quinazoline.
Kanatinib, Fanta, Nissola, Finney.
Sorafeni
4- chloro -(2- (methylamino)-carbonyl)-pyridine 4-(4- aminophenoxy) -N- methylpyridinium amide
Immune inhibitor
FTY720 antidiabetic drug
Sigliptin
Duloxetine hydrochloride and its intermediates
Duloxetine hydrochloride
(s)-n, n- dimethyl -3- (naphthalene-1- alkoxy) -3- (thiophene -2- yl) propyl-1- amine (HCl) aliskiren and its intermediate aliskiren base.
(2S, 4S, 5S)-5- amino -N-(2- carbamoyl -2- methylpropyl)-4,5- dihydroxy -2- isopropyl valeramide (r)-3,6-diethoxy -2,5-dihydro -2- isopropyl pyrazine
2-(3- methoxypropoxy) -4-((R)-2- (bromomethyl) -3- methylbutyl) -65438+ o-methoxybenzene)
2- (aminomethyl) -2- methylpropionamide
(R)-3-(3- methylbutyryl) -4- benzyloxazolidine -2- one1-((s)-2-(bromomethyl) -3- methylbutoxy) methyl) benzene
Carbalatine and Its Intermediates
Kabalatine tartrate cabalatine base
N- ethyl -N- methylaminoformyl chloride 3-[ 1- (dimethylamino) ethyl] phenol (s)-3-( 1- (dimethylamino) ethyl) phenol
Rocuronium bromide and its intermediate rocuronium bromide
5α- androst -2- ene-17- one
2-(4- morpholinyl)-16-( 1- pyrrolidinyl) -5- androstane -3, 17- diol
Erasmus and its intermediate Erasmus
3- nitro -4- phenylmethoxyanisole 3- amino -4- phenylmethoxyanisole 3- methylsulfonamido -4- phenoxyanisole
α-amino -2- methoxy -4- methanesulfonamido -5- phenoxyacetophenone hydrochloride
Amino-lezanol and its intermediates
6- isopropyl -4- oxo -4H- 1- benzopyran -3- formaldehyde (substituted benzopyran -3- formaldehyde) 6- isopropyl -4- oxo -4H- 1- benzopyran -3- nitrile (substituted benzopyran -3- nitrile
Rosuvastatin calcium and its intermediate
4-(4- fluorophenyl) -6- isopropyl -2-(n- methyl -n- methylsulfonamido) pyrimidine -5- methyl formate 4-(4- fluorophenyl) -6- isopropyl -2-(n- methyl -n- methylsulfonamido) pyrimidine -5- methanol parent nuclear alcohol.
4-(4- fluorophenyl) -6- isopropyl -2-(N- methyl -N- methylsulfonylamino) pyrimidine -5- formaldehyde
(5S)- rosuvastatin condensate ethyl rosuvastatin ethyl ester
(3R)- rosuvastatin condensate methyl ester rosuvastatin methyl ester
3- tert-butyldimethylsiloxane glutaric anhydride
(3R)- tert-butyldimethylsiloxyglutarate monomethyl ester
1- ethoxycarbonyl -5- methyl -(3R)- tert-butyldimethylsiloxy glutarate (3R)- tert-butyldimethylsiloxy -5- oxo -6- triphenylphosphine nonanoate methyl ester
[(4R-6S)-6-[ (acetoxy) methoxy]-2,2-dimethyl-1, 3- dioxane -4- yl] tert-butyl acetate side chain
Pitavastatin calcium and its intermediate
2- cyclopropyl -4-(4- fluorophenyl) quinoline -3- methanol 2- cyclopropyl -4-(4- fluorophenyl) quinoline -3- formaldehyde (E)-3-[2- cyclopropyl -4-(4- fluorophenyl) -3- quinoline -2- acrylonitrile.
(E)-3-[2- cyclopropyl -4-(4- fluorophenyl) -3- quinoline -2- acrolein (E)-(5s)-7-[2- cyclopropyl -4-(4- fluorophenyl) -3- quinoline] -5- hydroxy -3-.
Erdosteine and its intermediates
DL- N- chloroacetyl homocysteine thiolactone esmolol hydrochloride and its intermediate
N-(2,6-xylyl) N-(2-chloroacetamide
N-(2,6-dimethylphenyl)-1-( 1- piperazine) acetamide ranolazine ether
Ranolazine hydrochloride
Betalol hydrochloride and its intermediates
1-[4-(2- hydroxyethyl) phenoxy]-2,3-propylene oxide
1-{(4-[2- (cyclopropyl methoxy)-ethyl]-phenoxy}-2,3-propylene oxide betaxolol-levobetaxolol.
Tomedin
Tomatin sodium
Amtolmetin guacil guaamitamine: 87344-06-7 and its intermediate atracurium maleate and its intermediate tetrahydropapaverine hydrochloride 1, 5- pentanediol diacrylate demethylated atracurium oxalate (R)- (-)- tetrahydropapaverine hydrochloride (1R,1)
Calcium levofolinate /L- calcium folinate 3- methylthiophene luminol and its sodium salt CAS: 52 1-3 1-3 decitabine and its intermediate timopril;
(2s, 6R)-6- amino -5- oxo -2-(2- thienyl) perhydro-1, 4- thiazopyridine (intermediate of timopril) (2s, 6R)-6- amino -2-2- (thienyl) -6544.