31251-41-9

Basic information

• Product Name: 8-Chloro-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-one
• Synonyms: 8-CHLORO-5,6-DIHYDRO-11H-BENZO[5,6]CYCLOHEPTA[1,2-B]PYRIDIN-11-ONE;8-CHLORO-10,11-DIHYDRO-4-AZA-5H-DIBENZO-(A,D)CYCLOHEPTAN-5-ONE;8-CHLORO-10,11-DIHYDRO-4-AZA-5H-BENZO[A,D] CYCLOHEPTAN-5-ONE;8-CHLORO-5,6-DIHYDRO-11H-BENZO-(5,6)-CYCLOHEPTA-(1,2-B)-PYRIMIDINE-11-ON;8-Chloro-10,11-dihydro-4-aza-5;8-chloro-10,11-dihydro-4-AZA-5H-benzo〔A,D〕cyclohepta-5-one;8-CHLORO-5,6-DIHYDRO-11H-BENZO[5,6]CYCLOHEPTA[1,2-B]PYRIMIDINE-11-ONE;4-Aza-8-chloro-10,11-dihydro-5H-benzo[a,d]cyclo-5-heptanone
• CAS NO: 31251-41-9
• Molecular Formula: C₁₄H₁₀ClNO
• Molecular Weight: 243.69
• EINECS: 700-257-5
• Product Categories: Aromatics Compounds;Aromatics;Heterocycles;Intermediates
• Mol File: 31251-41-9.mol
• Article Data: 12

Chemical Properties

• Melting Point: 90-92°C
• Boiling Point: 433.614 °C at 760 mmHg
• Flash Point: 216.042 °C
• Appearance: Yellow solid
• Density: 1.314 g/cm³
• Vapor Pressure: 0mmHg at 25°C
• Refractive Index: 1.632
• Storage Temp.: -20?C Freezer
• Solubility: Chloroform (Slightly), Methanol (Slightly)
• PKA: 3.14±0.20(Predicted)
• CAS DataBase Reference: 8-Chloro-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-one(CAS DataBase Reference)
• NIST Chemistry Reference: 8-Chloro-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-one(31251-41-9)
• EPA Substance Registry System: 8-Chloro-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-one(31251-41-9)

Safety Data

• Hazard Codes: Xi
• Hazardous Substances Data: 31251-41-9(Hazardous Substances Data)

Usage

Chemical Properties

Yellow Solid

Uses

Different sources of media describe the Uses of 31251-41-9 differently. You can refer to the following data:
1. Loratadine intermediate. Loratidine impurity C.
2. 8-Chloro-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-one (Loratadine EP Impurity B; Loratadine USP Related Compound C) is a Loratadine intermediate. Loratidine impurity C.

InChI:InChI=1/C14H10ClNO/c15-11-5-6-12-10(8-11)4-3-9-2-1-7-16-13(9)14(12)17/h1-2,5-8H,3-4H2

Synthetic route

3-[2-(3-chlorophenyl)ethyl]-2-pyridine-carbonitrile (31255-57-9) → 8-chloro-5,6-dihydro-11H-Benzo[5,6]cyclohepta[1,2-b]pyridin-11-one (31251-41-9)

Conditions	Yield
Stage #1: 3-[2-(3-chlorophenyl)ethyl]-2-pyridine-carbonitrile With trifluorormethanesulfonic acid at 60℃; for 1h; Stage #2: With hydrogenchloride In water at 20℃; for 1h; Heating / reflux;	94%
With PPA at 200℃;	45%
With PPA Heating;

3-[2-(5-chloro-2-iodo-phenyl)-ethyl]-pyridine-2-carboxylic acid methyl-phenyl-amide (251353-79-4) → 8-chloro-5,6-dihydro-11H-Benzo[5,6]cyclohepta[1,2-b]pyridin-11-one (31251-41-9)

Conditions	Yield
With n-butyllithium In tetrahydrofuran; cyclohexane at -78℃; for 0.166667h;	91%
With n-butyllithium In tetrahydrofuran; cyclohexane at -78℃; for 0.166667h;	78%

C14H11ClN2 → 8-chloro-5,6-dihydro-11H-Benzo[5,6]cyclohepta[1,2-b]pyridin-11-one (31251-41-9)

Conditions	Yield
With water at 0 - 35℃; for 25 - 35h;	76.4%

C14H11Cl2NO → 8-chloro-5,6-dihydro-11H-Benzo[5,6]cyclohepta[1,2-b]pyridin-11-one (31251-41-9)

Conditions	Yield
With aluminum (III) chloride In carbon disulfide	40%

2-iodoyl-3,5-dichlorobenzoic acid (15396-37-9) → 8-chloro-5,6-dihydro-11H-Benzo[5,6]cyclohepta[1,2-b]pyridin-11-one (31251-41-9)

Conditions	Yield
Multi-step reaction with 5 steps 1.1: 121 g / (MeO)3B; BH3*Me2S / tetrahydrofuran / 18 h / 20 °C 2.1: PPh3; Br2 / acetonitrile / 1 h / 20 °C 3.1: LDA; t-BuOMe / various solvent(s); tetrahydrofuran / -30 - 0 °C 4.1: NaH / dimethylformamide / 1 h / 0 °C 4.2: 10 g / dimethylformamide / 0.25 h / 0 °C 5.1: 91 percent / n-BuLi / tetrahydrofuran; cyclohexane / 0.17 h / -78 °C View Scheme

5-chloro-2-iodobenzyl alcohol (82386-90-1) → 8-chloro-5,6-dihydro-11H-Benzo[5,6]cyclohepta[1,2-b]pyridin-11-one (31251-41-9)

Conditions	Yield
Multi-step reaction with 4 steps 1.1: PPh3; Br2 / acetonitrile / 1 h / 20 °C 2.1: LDA; t-BuOMe / various solvent(s); tetrahydrofuran / -30 - 0 °C 3.1: NaH / dimethylformamide / 1 h / 0 °C 3.2: 10 g / dimethylformamide / 0.25 h / 0 °C 4.1: 91 percent / n-BuLi / tetrahydrofuran; cyclohexane / 0.17 h / -78 °C View Scheme

2-(bromomethyl)-4-chloro-1-iodobenzene (82386-91-2) → 8-chloro-5,6-dihydro-11H-Benzo[5,6]cyclohepta[1,2-b]pyridin-11-one (31251-41-9)

Conditions	Yield
Multi-step reaction with 3 steps 1.1: LDA; t-BuOMe / various solvent(s); tetrahydrofuran / -30 - 0 °C 2.1: NaH / dimethylformamide / 1 h / 0 °C 2.2: 10 g / dimethylformamide / 0.25 h / 0 °C 3.1: 91 percent / n-BuLi / tetrahydrofuran; cyclohexane / 0.17 h / -78 °C View Scheme

3-[2-(5-chloro-2-iodo-phenyl)-ethyl]-pyridine-2-carboxylic acid phenylamide (251353-78-3) → 8-chloro-5,6-dihydro-11H-Benzo[5,6]cyclohepta[1,2-b]pyridin-11-one (31251-41-9)

Conditions	Yield
Multi-step reaction with 2 steps 1.1: NaH / dimethylformamide / 1 h / 0 °C 1.2: 10 g / dimethylformamide / 0.25 h / 0 °C 2.1: 91 percent / n-BuLi / tetrahydrofuran; cyclohexane / 0.17 h / -78 °C View Scheme

N-tert-butyl-3-methylpyridine-2-carboxamide (32998-95-1) → 8-chloro-5,6-dihydro-11H-Benzo[5,6]cyclohepta[1,2-b]pyridin-11-one (31251-41-9)

Conditions	Yield
Multi-step reaction with 3 steps 1: 1.) n-BuLi / 1.) THF, -40 deg C 2: POCl3 / Heating 3: PPA / Heating View Scheme

3-<2-(3-chlorophenyl)ethyl>-N-(1,1-dimethylethyl)-2-pyridinecarboxamide (107285-30-3) → 8-chloro-5,6-dihydro-11H-Benzo[5,6]cyclohepta[1,2-b]pyridin-11-one (31251-41-9)

Conditions	Yield
Multi-step reaction with 2 steps 1: POCl3 / Heating 2: PPA / Heating View Scheme

1-Chloro-3-chloromethyl-benzene (620-20-2) → 8-chloro-5,6-dihydro-11H-Benzo[5,6]cyclohepta[1,2-b]pyridin-11-one (31251-41-9)

Conditions	Yield
Multi-step reaction with 3 steps 1: 1.) n-BuLi / 1.) THF, -40 deg C 2: POCl3 / Heating 3: PPA / Heating View Scheme

3-[2-(3-Chlorophenyl)ethyl]-pyridine-2-carboxylic acid hydrochloride (255861-49-5) → 8-chloro-5,6-dihydro-11H-Benzo[5,6]cyclohepta[1,2-b]pyridin-11-one (31251-41-9)

Conditions	Yield
Stage #1: 3-[2-(3-Chlorophenyl)ethyl]-pyridine-2-carboxylic acid hydrochloride With thionyl chloride at 30 - 60℃; Stage #2: aluminum (III) chloride In 1,2-dichloro-ethane at -5 - 20℃;

N-phenyl-3-[2-(3-chlorophenyl)ethyl]-2-pyridine carboxamide (271252-79-0) + phosphorus pentachloride (10026-13-8, 874483-75-7) + pyrographite (7440-44-0) → 8-chloro-5,6-dihydro-11H-Benzo[5,6]cyclohepta[1,2-b]pyridin-11-one (31251-41-9)

Conditions	Yield
aluminium trichloride In hexane; dichloromethane; toluene	44.2 g (61%)

N-phenyl-3-[2-(3-chlorophenyl)ethyl]-2-pyridine carboxamide (271252-79-0) + pyrographite (7440-44-0) → 8-chloro-5,6-dihydro-11H-Benzo[5,6]cyclohepta[1,2-b]pyridin-11-one (31251-41-9)

Conditions	Yield
With trichlorophosphate In hexane; water; chlorobenzene	44.1 g (50.8%)

3-(2-(3-chlorophenyl)ethenyl)pyridine-2-carboxylate → 8-chloro-5,6-dihydro-11H-Benzo[5,6]cyclohepta[1,2-b]pyridin-11-one (31251-41-9)

Conditions	Yield
Multi-step reaction with 4 steps 1: 5%-palladium/activated carbon; hydrogen / ethyl acetate / 4 h / 760.05 Torr 2: sodium hydroxide; water / ethanol / 48 h 3: thionyl chloride 4: aluminum (III) chloride / carbon disulfide View Scheme

methyl 3-(2-(3-chlorophenyl)ethanyl)pyridine-2-carboxylate → 8-chloro-5,6-dihydro-11H-Benzo[5,6]cyclohepta[1,2-b]pyridin-11-one (31251-41-9)

Conditions	Yield
Multi-step reaction with 3 steps 1: sodium hydroxide; water / ethanol / 48 h 2: thionyl chloride 3: aluminum (III) chloride / carbon disulfide View Scheme

3-(2-(3-chlorophenyl)ethanyl)pyridine-2-carboxylic acid → 8-chloro-5,6-dihydro-11H-Benzo[5,6]cyclohepta[1,2-b]pyridin-11-one (31251-41-9)

Conditions	Yield
Multi-step reaction with 2 steps 1: thionyl chloride 2: aluminum (III) chloride / carbon disulfide View Scheme

isopropyl 3-(2-(3-chlorophenyl)ethenyl)pyridine-2-carboxylate → 8-chloro-5,6-dihydro-11H-Benzo[5,6]cyclohepta[1,2-b]pyridin-11-one (31251-41-9)

Conditions	Yield
Multi-step reaction with 4 steps 1: 5%-palladium/activated carbon; hydrogen / ethyl acetate / 48 h / 760.05 Torr 2: sodium hydroxide; water / ethanol / 5 h / Reflux 3: thionyl chloride 4: aluminum (III) chloride / carbon disulfide View Scheme

isopropyl 3-(2-(3-chlorophenyl)ethanyl)pyridine-2-carboxylate → 8-chloro-5,6-dihydro-11H-Benzo[5,6]cyclohepta[1,2-b]pyridin-11-one (31251-41-9)

Conditions	Yield
Multi-step reaction with 3 steps 1: sodium hydroxide; water / ethanol / 5 h / Reflux 2: thionyl chloride 3: aluminum (III) chloride / carbon disulfide View Scheme

C20H15ClN2 → 8-chloro-5,6-dihydro-11H-Benzo[5,6]cyclohepta[1,2-b]pyridin-11-one (31251-41-9)

Conditions	Yield
With water; sodium hydroxide In tetrahydrofuran at 80 - 90℃; pH=10-11;

8-chloro-5,6-dihydro-11H-Benzo[5,6]cyclohepta[1,2-b]pyridin-11-one (31251-41-9) → 8-Chloro-6,11-Dihydro-11-Hydroxy-5H-Benzo[5,6]-Cyclohepta[1,2-b]Pyridine (133330-72-0)

Conditions	Yield
Stage #1: 8-chloro-5,6-dihydro-11H-Benzo[5,6]cyclohepta[1,2-b]pyridin-11-one With sodium tetrahydroborate In methanol at 0 - 20℃; for 1h; Stage #2: With hydrogenchloride In methanol; water	100%
With sodium tetrahydroborate In methanol at 10 - 20℃; for 2.75h;	96.9%
With sodium tetrahydroborate In methanol a) 0 deg C, 2.5 h, b) from 0 deg C to 25 deg C, 1 h;

8-chloro-5,6-dihydro-11H-Benzo[5,6]cyclohepta[1,2-b]pyridin-11-one (31251-41-9) + (1-methyl-4-piperidyl)magnesium chloride (63463-36-5) → 8-chloro-6,11-dihydro-11-(1-methyl-4-piperidinyl)-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ol (38089-93-9)

Conditions	Yield
In tetrahydrofuran Reflux;	95%
With (trimethylsilyl)methylmagnesium chloride; lithium chloride; zinc(II) chloride In tetrahydrofuran; diethyl ether at 0℃; for 2h; Inert atmosphere;	90%
In tetrahydrofuran at -95 - -15℃; for 2 - 3h;	71.1%

8-chloro-5,6-dihydro-11H-Benzo[5,6]cyclohepta[1,2-b]pyridin-11-one (31251-41-9) → 5,6-Dihydro-11H-benzo<5,6>cyclohepta<1,2-b>pyridin-11-one (3964-73-6)

Conditions	Yield
With palladium on activated charcoal; hydrogen; triethylamine In tetrahydrofuran at 20℃; for 24h;	89%

8-chloro-5,6-dihydro-11H-Benzo[5,6]cyclohepta[1,2-b]pyridin-11-one (31251-41-9) + diethyl N-ethoxycarbonylpiperidine-4-phosphonate (216870-24-5) → C24H28ClN2O5P

Conditions	Yield
Stage #1: diethyl N-ethoxycarbonylpiperidine-4-phosphonate With n-butyllithium; diisopropylamine In tetrahydrofuran; hexane at -25 - -5℃; for 2h; Stage #2: 8-chloro-5,6-dihydro-11H-Benzo[5,6]cyclohepta[1,2-b]pyridin-11-one In tetrahydrofuran; hexane at -25 - -20℃; for 2h;	82%

8-chloro-5,6-dihydro-11H-Benzo[5,6]cyclohepta[1,2-b]pyridin-11-one (31251-41-9) + 1-methylpiperidin-2-one (931-20-4) → 3-(8-Chloro-11-hydroxy-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)-1-methyl-piperidin-2-one (212390-12-0)

Conditions	Yield
With n-butyllithium; diisopropylamine In tetrahydrofuran; hexane 1.) -78 deg C, 30 min; -78 deg C to -5 deg C, 60 min, 2.) -78 deg C, 1 h; -78 deg C to -10 deg C, 1 h;	76%

2-(4-formylphenyl)pyridine (127406-56-8) + 8-chloro-5,6-dihydro-11H-Benzo[5,6]cyclohepta[1,2-b]pyridin-11-one (31251-41-9) → C26H18ClN3

Conditions	Yield
With ammonium acetate; acetic acid for 10h; Reflux;	75%

8-chloro-5,6-dihydro-11H-Benzo[5,6]cyclohepta[1,2-b]pyridin-11-one (31251-41-9) + methyl 4-formylbenzoate (1571-08-0) → C23H17ClN2O2

Conditions	Yield
With ammonium acetate; acetic acid for 10h; Reflux;	75%

8-chloro-5,6-dihydro-11H-Benzo[5,6]cyclohepta[1,2-b]pyridin-11-one (31251-41-9) + 4-phenylsulfanyl-benzaldehyde (1208-88-4) → C27H19ClN2S

Conditions	Yield
With ammonium acetate; acetic acid for 8h; Reflux;	74%

8-chloro-5,6-dihydro-11H-Benzo[5,6]cyclohepta[1,2-b]pyridin-11-one (31251-41-9) + Phenanthrene-9-carboxaldehyde (4707-71-5) → C29H19ClN2

Conditions	Yield
With ammonium acetate; acetic acid for 7h; Reflux;	74%

8-chloro-5,6-dihydro-11H-Benzo[5,6]cyclohepta[1,2-b]pyridin-11-one (31251-41-9) + triethyl phosphite (122-52-1) → C18H21ClNO3P

Conditions	Yield
With toluene-4-sulfonic acid In toluene at 20℃; for 24h;	73.8%

4-chloro-1-methylpiperidine (5570-77-4) + 8-chloro-5,6-dihydro-11H-Benzo[5,6]cyclohepta[1,2-b]pyridin-11-one (31251-41-9) → 8-chloro-6,11-dihydro-11-(1-methyl-4-piperidinyl)-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ol (38089-93-9)

Conditions	Yield
Stage #1: 4-chloro-1-methylpiperidine With magnesium; ethylene dibromide In tetrahydrofuran at 20 - 48℃; Stage #2: 8-chloro-5,6-dihydro-11H-Benzo[5,6]cyclohepta[1,2-b]pyridin-11-one In tetrahydrofuran at -80 - -70℃; for 2 - 3h; Product distribution / selectivity;	73.6%

8-chloro-5,6-dihydro-11H-Benzo[5,6]cyclohepta[1,2-b]pyridin-11-one (31251-41-9) + 4-cyanobenzaldehyde (105-07-7) → C22H14ClN3

Conditions	Yield
With ammonium acetate; acetic acid for 6h; Reflux;	73%

8-chloro-5,6-dihydro-11H-Benzo[5,6]cyclohepta[1,2-b]pyridin-11-one (31251-41-9) + 2,6-dibromobenzaldehyde (67713-23-9) → C21H13Br2ClN2

Conditions	Yield
With ammonium acetate; acetic acid for 6h; Reflux;	73%

8-chloro-5,6-dihydro-11H-Benzo[5,6]cyclohepta[1,2-b]pyridin-11-one (31251-41-9) + 4-styrylbenzaldehyde (32555-96-7) → C29H21ClN2

Conditions	Yield
With ammonium acetate; acetic acid for 8h; Reflux;	72%

8-chloro-5,6-dihydro-11H-Benzo[5,6]cyclohepta[1,2-b]pyridin-11-one (31251-41-9) + 9H-fluorene-2-carbaldehyde (30084-90-3) → C28H19ClN2

Conditions	Yield
With ammonium acetate; acetic acid for 6h; Reflux;	71%

8-chloro-5,6-dihydro-11H-Benzo[5,6]cyclohepta[1,2-b]pyridin-11-one (31251-41-9) + N-(4-formylphenyl)carbazole (110677-45-7) → C33H22ClN3

Conditions	Yield
With ammonium acetate; acetic acid for 10h; Reflux;	70%

8-chloro-5,6-dihydro-11H-Benzo[5,6]cyclohepta[1,2-b]pyridin-11-one (31251-41-9) + para-methanesulfonylbenzaldehyde (5398-77-6) → C22H17ClN2O2S

Conditions	Yield
With ammonium acetate; acetic acid for 10h; Reflux;	70%

8-chloro-5,6-dihydro-11H-Benzo[5,6]cyclohepta[1,2-b]pyridin-11-one (31251-41-9) + 6-fluorochromone-3-carboxaldehyde (69155-76-6) → C24H14ClFN2O2

Conditions	Yield
With ammonium acetate; acetic acid for 8h; Reflux;	70%

8-chloro-5,6-dihydro-11H-Benzo[5,6]cyclohepta[1,2-b]pyridin-11-one (31251-41-9) + 2,6-dichlorobenzaldehyde (83-38-5) → C21H13Cl3N2

Conditions	Yield
With ammonium acetate; acetic acid for 6h; Reflux;	69%

1H-pyrrolo[2,3-b]pyridin-3-carbaldehyde (4649-09-6) + 8-chloro-5,6-dihydro-11H-Benzo[5,6]cyclohepta[1,2-b]pyridin-11-one (31251-41-9) → C22H15ClN4

Conditions	Yield
With ammonium acetate; acetic acid for 8h; Reflux;	68%

8-chloro-5,6-dihydro-11H-Benzo[5,6]cyclohepta[1,2-b]pyridin-11-one (31251-41-9) + 4-(Methylthio)benzaldehyde (3446-89-7) → C22H17ClN2S

Conditions	Yield
With ammonium acetate; acetic acid for 7h; Reflux;	68%

4-benzooxazol-2-yl-benzaldehyde (27395-93-3) + 8-chloro-5,6-dihydro-11H-Benzo[5,6]cyclohepta[1,2-b]pyridin-11-one (31251-41-9) → C28H18ClN3O

Conditions	Yield
With ammonium acetate; acetic acid for 7h; Reflux;	68%

2,2'-bithiophene-5-carboxaldehyde (3779-27-9) + 8-chloro-5,6-dihydro-11H-Benzo[5,6]cyclohepta[1,2-b]pyridin-11-one (31251-41-9) → C23H15ClN2S2

Conditions	Yield
With ammonium acetate; acetic acid for 10h; Reflux;	67%

8-chloro-5,6-dihydro-11H-Benzo[5,6]cyclohepta[1,2-b]pyridin-11-one (31251-41-9) + 4-(diphenylamino)benzaldehyde (4181-05-9) → C33H24ClN3

Conditions	Yield
With ammonium acetate; acetic acid for 10h; Reflux;	66%

8-chloro-5,6-dihydro-11H-Benzo[5,6]cyclohepta[1,2-b]pyridin-11-one (31251-41-9) + phosphorous acid trimethyl ester (121-45-9) → dimethyl (8-chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)phosphonate

Conditions	Yield
With phosphoric acid In chloroform at 20℃; for 12h;	65%

3-(2-cyclopropyl-4-(4-fluorophenyl)-3-quinolinyl)prop-2-enal + 8-chloro-5,6-dihydro-11H-Benzo[5,6]cyclohepta[1,2-b]pyridin-11-one (31251-41-9) → C35H25ClFN3

Conditions	Yield
With ammonium acetate; acetic acid for 7h; Reflux;	65%

Upstream product

• 31255-57-9 3-[2-(3-chlorophenyl)ethyl]-2-pyridine-carbonitrile 
• 620-20-2 1-Chloro-3-chloromethyl-benzene 
• 271252-79-0 N-phenyl-3-[2-(3-chlorophenyl)ethyl]-2-pyridine carboxamide 
• 10026-13-8 phosphorus pentachloride 
• 7440-44-0 pyrographite 
• 255861-49-5 3-[2-(3-Chlorophenyl)ethyl]-pyridine-2-carboxylic acid hydrochloride 
• 107285-30-3 3-<2-(3-chlorophenyl)ethyl>-N-(1,1-dimethylethyl)-2-pyridinecarboxamide 
• 32998-95-1 N-tert-butyl-3-methylpyridine-2-carboxamide 
• 251353-78-3 3-[2-(5-chloro-2-iodo-phenyl)-ethyl]-pyridine-2-carboxylic acid phenylamide 
• 82386-91-2 2-(bromomethyl)-4-chloro-1-iodobenzene 
• 82386-90-1 5-chloro-2-iodobenzyl alcohol 
• 15396-37-9 2-iodoyl-3,5-dichlorobenzoic acid 
• 251353-79-4 3-[2-(5-chloro-2-iodo-phenyl)-ethyl]-pyridine-2-carboxylic acid methyl-phenyl-amide 

Downstream Products

• 183554-46-3 1-Benzyl-3-(8-chloro-11-hydroxy-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)-pyrrolidin-2-one 
• 38089-93-9 8-chloro-6,11-dihydro-11-(1-methyl-4-piperidinyl)-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ol 
• 1373612-35-1 4-(8-chloro-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene)-N-(2-methoxyphenyl)-1-piperidinecarbothioamide 
• 1373612-32-8 4-(8-chloro-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene)-N-cyclohexyl-1-piperidinecarbothioamide 
• 1373612-33-9 4-(8-chloro-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene)-N-phenyl-1-piperidinecarbothioamide 
• 1373612-34-0 4-(8-chloro-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene)-N-(2-methylphenyl)-1-piperidinecarbothioamide 
• 100643-71-8 descarboethoxyloratadine 
• 79794-75-5 loratadine 
• 38092-89-6 N-methyldesloratadine 

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Method for preparing anti-allergic rhinitis medicine loratadine intermediate

The invention belongs to the technical field of chemical medicine preparation and particularly relates to a method for preparing an anti-allergic rhinitis medicine, namely a loratadine intermediate. According to the method, ammonium meta-tungstate is adopted as a WO3 precursor, ZrOC12*8H2O is adopted as a ZrO2 precursor, and a WO3/ZrO2 solid super-strong acid is supported by sulfamic acid graftingmodified silica gel, and then a silica gel supported solid acid is prepared. As 8-chlorine-5,6-dihydro-11H-benzo[5,6] cycloheptane[1,2-b] pyridine-11-ketone is prepared from the novel silica gel supported solid acid through catalysis, the problem of excessive wastewater is overcome, the environment protection burden is alleviated, and the reaction yield can be increased.

Aza-analogue dibenzepinone scaffolds as p38 mitogen-activated protein kinase inhibitors:Design, synthesis, and biological data of inhibitors with improved physicochemical properties

We recently described a promising novel class of p38 mitogen activated protein (MAP) kinase inhibitors with dibenzepinone-scaffolds. To optimize their physicochemical properties, characterized by calculated log P values and measured lipophilicity (chromatographic hydrophobicity index=CHI), we synthesized aza-analogue dibenzepinones. Here, we present the synthesis and biological data of compounds with the novel aza-dibenzepinone scaffolds. Although these aza-analogues revealed an improved aqueous solubility, introduction of nitrogen was not effective in the p38 MAPK enzyme assay.

A PROCESS FOR PREPARING BENZOCYCLOHEPTAPYRIDIN-11-ONES

A novel method for generating dianions using 3-methylpyridine-2-carboxylic acid derivatives of formula (V) or using their corresponding alkali metal salts of formula (VI), preferably from their lithium salt (Scheme 3) is described. The substituents R, R, R, R, R, R and R in Scheme 3 are defined as herein described above. Preferably the substituents are selected from one or more of hydrogen, halogen or C1-C6 alkyl groups. M is represented by any alkali metal ion, preferably lithium.