5308-25-8

Basic information

• Product Name: 1-Ethylpiperazine
• Synonyms: 1-ethyl-piperazin;Piperazine, 1-ethyl-;ETHYLPIPERAZINE-N;LABOTEST-BB LTBB000704;1-ETHYLPIPERAZINE;AKOS BBS-00003610;N-ETHYLPIPERAZINE;NEPRZ
• CAS NO: 5308-25-8
• Molecular Formula: C₆H₁₄N₂
• Molecular Weight: 114.19
• EINECS: 226-166-6
• Product Categories: Piperidines, Piperidones, Piperazines;Piperaizine;Piperazines;Building Blocks;Heterocyclic Building Blocks;Building Blocks;C4 to C8;Chemical Synthesis;Heterocyclic Building Blocks
• Mol File: 5308-25-8.mol
• Article Data: 17

Chemical Properties

• Melting Point: -60 °C
• Boiling Point: 157 °C(lit.)
• Flash Point: 110 °F
• Appearance: Clear colorless to yellow/Liquid
• Density: 0.899 g/mL at 25 °C(lit.)
• Vapor Pressure: 2.96mmHg at 25°C
• Refractive Index: n20/D 1.469(lit.)
• Storage Temp.: Flammables area
• Solubility: soluble
• PKA: 9.27±0.10(Predicted)
• Water Solubility: soluble
• Sensitive: Air Sensitive
• BRN: 102971
• CAS DataBase Reference: 1-Ethylpiperazine(CAS DataBase Reference)
• NIST Chemistry Reference: 1-Ethylpiperazine(5308-25-8)
• EPA Substance Registry System: 1-Ethylpiperazine(5308-25-8)

Safety Data

• Hazard Codes: Xi,Hazard
• Statements: 36/37/38-10
• Safety Statements: 26-36
• RIDADR: UN 1993 3/PG 3
• WGK Germany: 1
• RTECS: TM0815500
• F: 10-34
• HazardClass: 3
• PackingGroup: III
• Hazardous Substances Data: 5308-25-8(Hazardous Substances Data)

Usage

Chemical Properties

clear colorless to yellow liquid

Uses

Different sources of media describe the Uses of 5308-25-8 differently. You can refer to the following data:
1. 1-Ethylpiperazine is used in the synthesis of 2-(2-methoxy-5-((4-methylpiperazin-1-yl)sulfonyl)phenyl)-1H-benzo[d]imidazole hydrochloride and 2-(5-((4-ethylpiperazin-1-yl)sulfonyl)-2-methoxyphenyl)-1H-benzo[d]imidazole hydrochloride. It is also employed as an intermediate in veterinary medicine, especially in the production of ciproflmoxacin ethyl. Further, it serves as a precursor to prepare dyes.
2. 1-Ethylpiperazine may be used in the preparation of 2-(2-methoxy-5-((4-methylpiperazin-1-yl)sulfonyl)phenyl)-1H-benzo[d]imidazole hydrochloride and 2-(5-((4-ethylpiperazin-1-yl)sulfonyl)-2-methoxyphenyl)-1H-benzo[d]imidazole hydrochloride.

Synthesis Reference(s)

The Journal of Organic Chemistry, 22, p. 713, 1957 DOI: 10.1021/jo01357a621

Flammability and Explosibility

Flammable

InChI:InChI=1/C6H14N2/c1-2-8-5-3-7-4-6-8/h7H,2-6H2,1H3/p+2

Synthetic route

C11H22N2O2 → 4-ethylpiperazine (5308-25-8)

Conditions	Yield
With trifluoroacetic acid at 20℃; for 0.0833333h;	94%

piperazine (110-85-0) + chloroethane (75-00-3) → 4-ethylpiperazine (5308-25-8) + 1,4-diethylpiperazine (6483-50-7)

Conditions	Yield
	A 20% B 55%

4-ethyl-1-formylpiperazine (21863-75-2) → 4-ethylpiperazine (5308-25-8)

Conditions	Yield
With hydrogenchloride

ethyl bromide (74-96-4) + piperazine hydrochloride (7542-23-6) → 4-ethylpiperazine (5308-25-8)

Conditions	Yield
With ethanol

4-ethyl-piperazine-1-carboxylic acid ethyl ester (98951-41-8) → 4-ethylpiperazine (5308-25-8)

Conditions	Yield
With hydrogen bromide; acetic acid
With hydrogenchloride

EtN(CH2CN)2 (24426-42-4) → 4-ethylpiperazine (5308-25-8)

Conditions	Yield
With nickel; platinum; benzene at 44℃; Hydrogenation;

ethanamine hydrochloride (557-66-4) + morpholin hydrochloride (10024-89-2) → 4-ethylpiperazine (5308-25-8)

Conditions	Yield
at 265℃;
at 265℃;

diethyl amine hydrochloride (660-68-4) + morpholin hydrochloride (10024-89-2) → 4-ethylpiperazine (5308-25-8)

Conditions	Yield
at 250℃;

1-benzyl-4-ethylpiperazine dihydrochloride → 4-ethylpiperazine (5308-25-8)

Conditions	Yield
With palladium on activated charcoal Hydrogenation;

bis-(2-chloroethyl)amine hydrochloride (821-48-7) + ethylamine (75-04-7) → 4-ethylpiperazine (5308-25-8)

Conditions	Yield
at 130℃;

ethylamine (75-04-7) + 2,2'-iminobis[ethanol] (111-42-2) → 4-ethylpiperazine (5308-25-8)

Conditions	Yield
With nickel at 225℃;

1-ethyl-4-<4-chloro-benzyl>-piperazine dihydrobromide → 4-ethylpiperazine (5308-25-8)

Conditions	Yield
With palladium on activated charcoal Hydrogenation;

1-ethyl-4-<4-nitroso-phenyl>-piperazine → 4-ethylpiperazine (5308-25-8)

Conditions	Yield
With sulfur dioxide anschliessend mit wss.KOH;

2-<2-diethylamino-ethylamino>-ethanol dihydrochloride → 4-ethylpiperazine (5308-25-8)

Conditions	Yield
at 260℃;

ethanamine hydrochloride (557-66-4) + 1-ethyl-piperazine hydrochloride → 4-ethylpiperazine (5308-25-8)

Conditions	Yield
at 260℃;

diethyl amine hydrochloride (660-68-4) + 1-ethyl-piperazine hydrochloride → 4-ethylpiperazine (5308-25-8)

Conditions	Yield
at 250℃;

ethyl-bis-<2-hydroxy-ethyl>-amine hydrochloride → 4-ethylpiperazine (5308-25-8)

Conditions	Yield
With ammonium chloride at 260℃;

N-ethyl-piperazine-N'-carboxylic acid ethyl ester → 4-ethylpiperazine (5308-25-8)

Conditions	Yield
With hydrogenchloride

propan-1-ol-3-amine (156-87-6) → morpholine (110-91-8) + 4-ethylpiperazine (5308-25-8) + 2-Methylpyrazine (109-08-0) + ethanol (64-17-5) + 1-amino-2-propene (107-11-9) + 2-Methylaziridine (75-55-8, 41927-28-0, 76612-76-5, 76612-77-6, 205537-16-2) + propane, methylamine, ethylamine, 2,5-dimethylpyrrole

Conditions	Yield
tungsten(VI) oxide at 400℃; Product distribution; other temperatures;

(4-ethyl-1-piperazinyl)(phenyl)methanone (60787-02-2) → 4-ethylpiperazine (5308-25-8)

Conditions	Yield
With hydrogenchloride Heating;

piperazine (110-85-0) + Reaxys ID: 11370776 + ethanol (64-17-5) → 4-ethylpiperazine (5308-25-8) + 1,4-diethylpiperazine (6483-50-7)

Conditions	Yield
Stage #1: With hydrogen at 200℃; for 3h; Stage #2: piperazine; ethanol With hydrogen at 200℃; under 7500.75 Torr; for 8h; Product distribution / selectivity;

blonanserin → 4-ethylpiperazine (5308-25-8) + 2-(piperazine-1-yl)-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydrocycloocta[b]pyridine + C21H28FN3 + C23H28FN3O2

Conditions	Yield
at 40℃; UV-irradiation;

N-ethylethane-1,2-diamine (110-72-5) + Glyoxal (131543-46-9) → 4-ethylpiperazine (5308-25-8)

Conditions	Yield
With glucose-6-phosphate dehydrogenase; glucose-6-phosphate; Myxococcus stipitatus R-selective imine reductase; NADPH; magnesium chloride In aq. phosphate buffer at 25℃; for 4h; pH=7; Enzymatic reaction;

2-hydroxy-1-(piperazin-1-yl)ethanone → 4-ethylpiperazine (5308-25-8) + 1-(2-hydroxyethyl)piperazine (103-76-4)

Conditions	Yield
With hydrogen In toluene at 200℃; under 37503.8 Torr; Solvent; Reagent/catalyst; Temperature; Pressure; Autoclave; Sealed tube;	A 68.63 g B 164.81 g

4-ethylpiperazine (5308-25-8) + ethyl 2-chloro-5-(chlorosulfonyl)nicotinate (334708-07-5) → Ethyl 2-chloro-5-(4-ethyl-1-piperazinylsulfonyl) nicotinoate (334708-08-6)

Conditions	Yield
With triethylamine In toluene at 10 - 20℃; for 19.5h;	100%
With triethylamine In ethyl acetate at 0 - 22℃; for 1.5h;
With triethylamine In ethyl acetate at 0 - 22℃; for 1.5h;

4-ethylpiperazine (5308-25-8) + ethyl 4-(1-bromoethyl)benzoic acid (221279-14-7) → 4-(4-ethyl piperazin-1-ylmethyl)-benzoic acid ethyl ester (1044872-36-7)

Conditions	Yield
In tetrahydrofuran at 20℃; for 16h;	100%

4-ethylpiperazine (5308-25-8) + Ethyl 4-(bromomethyl)benzoate (26496-94-6) → 4-(4-ethyl piperazin-1-ylmethyl)-benzoic acid ethyl ester (1044872-36-7)

Conditions	Yield
In tetrahydrofuran at 20℃; for 16h;	100%
In tetrahydrofuran at 20℃; for 16h;

4-ethylpiperazine (5308-25-8) + methyl 2-(chloromethyl)-4-(2-methyl-1H-indol-3-yl)-4H-chromene-3-carboxylate (1257865-27-2) → methyl 2-[(4-ethylpiperazin-1-yl)methyl]-4-(2-methyl-1H-indol-3-yl)-4H-chromene-3-carboxylate (1257865-29-4)

Conditions	Yield
In acetonitrile at 25℃; for 20h;	100%

4-ethylpiperazine (5308-25-8) + 3-(2,6-difluoro-3,5-dimethoxyphenyl)-1-methyl-2-oxo-7-(phenylsulfonyl)-2,3,4,7-tetrahydro-1H-pyrrolo[3‘,2‘:5,6]pyrido[4,3-d]pyrimidine-8-carbaldehyde (1513859-71-6) → 3-(2,6-difluoro-3,5-dimethoxyphenyl)-8-[(4-ethylpiperazin-1-yl)methyl]-1-methyl-7-(phenylsulfonyl)-1,3,4,7-tetrahydro-2H-pyrrolo[3‘,2‘:5,6]pyrido[4,3-d]pyrimidin-2-one (1513859-72-7)

Conditions	Yield
With sodium tris(acetoxy)borohydride; trifluoroacetic acid In dichloromethane at 0℃; for 2h;	100%

4-ethylpiperazine (5308-25-8) + C18H21ClO → 1-ethyl-4-[4-(2-tricyclo[3.3.1.13,7]decyl)phenylacetyl]piperazine

Conditions	Yield
In tetrahydrofuran at 20℃; for 12h;	100%

4-ethylpiperazine (5308-25-8) + N-(4-bromo-2-nitrophenyl)-N-tert-butoxycarbonylcarbamic acid tert-butyl ester (1228392-59-3) → tert-butyl (4-(4-ethylpiperazin-1-yl)-2-nitrophenyl)carbamate

Conditions	Yield
With chloro(2-dicyclohexylphosphino-2′,6′-di-i-propoxy-1,1′-biphenyl)(2′-amino-1,1′-biphenyl-2-yl)-palladium(II); caesium carbonate In toluene at 95 - 105℃; Inert atmosphere;	100%
With tris-(dibenzylideneacetone)dipalladium(0); caesium carbonate; XPhos In toluene at 110℃; for 8h; Inert atmosphere;	4.8 g

4-ethylpiperazine (5308-25-8) + 5-chloro-6-ethoxycarbonylpyridine-3-carboxylic acid (1198475-22-7) → ethyl 3-chloro-5-(4-ethylpiperazine-1-carbonyl)picolinate

Conditions	Yield
Stage #1: 5-chloro-6-ethoxycarbonylpyridine-3-carboxylic acid With benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; triethylamine In N,N-dimethyl-formamide at 20℃; for 0.0833333h; Stage #2: 4-ethylpiperazine In N,N-dimethyl-formamide at 20℃;	100%

4-ethylpiperazine (5308-25-8) + 4-Methoxyphenyl isocyanate (5416-93-3) → 4-ethyl-N-(4-methoxyphenyl)piperazine-1-carboxamide

Conditions	Yield
In diethyl ether at 20℃; for 5h;	99.7%

4-ethylpiperazine (5308-25-8) + 3-methoxyphenyl isocyanate (18908-07-1) → 4-ethyl-N-(3-methoxyphenyl)piperazine-1-carboxamide

Conditions	Yield
In diethyl ether at 20℃; for 5h;	99.7%

4-ethylpiperazine (5308-25-8) + 1-(3-bromopropoxy)-4-nitrobenzene (13094-50-3) → 1-ethyl-4-(3-(4-nitrophenoxy)propyl)piperazine

Conditions	Yield
With potassium carbonate In acetonitrile for 17h; Reflux;	99.6%

4-ethylpiperazine (5308-25-8) + 1-(4-bromobutoxy)-4-nitrobenzene (55502-03-9) → 1-ethyl-4-(4-(4-nitrophenoxy)butyl)piperazine

Conditions	Yield
With potassium carbonate In acetonitrile for 17h; Reflux;	99.5%

4-ethylpiperazine (5308-25-8) + 1-fluoro-3-isocyanatobenzene (404-71-7) → 4-ethyl-N-(3-fluorophenyl)piperazine-1-carboxamide

Conditions	Yield
In diethyl ether at 20℃; for 5h;	99.5%

4-ethylpiperazine (5308-25-8) + para-fluorophenyl isocyanate (1195-45-5) → 4-ethyl-N-(4-fluorophenyl)piperazine-1-carboxamide

Conditions	Yield
In diethyl ether at 20℃; for 5h;	99.5%

4-ethylpiperazine (5308-25-8) + 3-(4-methoxyphenyl)-1-chloromethylisoquinoline → 3-(4-methoxyphenyl)-(1-(4-ethylpiperazin-1-yl)methyl)isoquinoline

Conditions	Yield
	99%

4-ethylpiperazine (5308-25-8) + 4-(bromomethyl)-3-(trifluoromethyl)benzoic acid methyl ester (863248-28-6) → methyl 4-((4-ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)benzoate

Conditions	Yield
With caesium carbonate In N,N-dimethyl-formamide at 80℃; for 3h;	99%

4-ethylpiperazine (5308-25-8) + formaldehyd (50-00-0) → 1-ethyl-4-methylpiperazine dihydrochloride (73993-07-4)

Conditions	Yield
Stage #1: 4-ethylpiperazine; formaldehyd With hydrogen In tetrahydrofuran at 120℃; under 3750.38 Torr; for 9h; Autoclave; Stage #2: With hydrogenchloride In water	99%

4-ethylpiperazine (5308-25-8) + 1-(6-bromopyridin-3-yl)propyl methanesulfonate → 1-(1-(6-bromopyridin-3-yl)propyl)-4-ethylpiperazine

Conditions	Yield
With N-ethyl-N,N-diisopropylamine In N,N-dimethyl-formamide at 80℃; for 12h; Inert atmosphere;	99%

4-ethylpiperazine (5308-25-8) + 2-chloro-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydrocycloocta[b]pyridine (132813-14-0) → blonanserin

Conditions	Yield
With N-ethyl-N,N-diisopropylamine In N,N-dimethyl-formamide at 70℃; for 5h;	98.6%
Stage #1: 4-ethylpiperazine; 2-chloro-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydrocycloocta[b]pyridine With sodium t-butanolate In toluene at 10℃; under 75.0075 Torr; for 0.0333333h; Inert atmosphere; Stage #2: With palladium diacetate; triphenylphosphine In toluene at 70℃; under 75.0075 Torr; for 7h; Reagent/catalyst; Solvent; Temperature; Inert atmosphere;	89.12%
With 2,2'-bis-(diphenylphosphino)-1,1'-binaphthyl; bis(dibenzylideneacetone)-palladium(0); sodium t-butanolate In toluene at 75 - 85℃; for 3h; Large scale;	88%

4-ethylpiperazine (5308-25-8) + tetramethylorthosilicate (681-84-5) → bis(N-ethyl)piperazinyl dimethoxysilane

Conditions	Yield
Stage #1: 4-ethylpiperazine With n-butyllithium In tetrahydrofuran at 20℃; for 1h; Inert atmosphere; Cooling with ice; Stage #2: tetramethylorthosilicate In tetrahydrofuran at 0 - 20℃; for 6h; Inert atmosphere;	98.6%
Stage #1: 4-ethylpiperazine With n-butyllithium In hexane at 10℃; for 1h; Inert atmosphere; Stage #2: tetramethylorthosilicate In hexane for 17h; Inert atmosphere;

4-ethylpiperazine (5308-25-8) + isopropyl trimethoxy silane (14346-37-3) → ethylpiperazine isopropyl dimethoxy silane

Conditions	Yield
Stage #1: 4-ethylpiperazine With n-butyllithium In tetrahydrofuran at 20℃; for 2h; Inert atmosphere; Cooling with ice; Stage #2: isopropyl trimethoxy silane In tetrahydrofuran at 0 - 20℃; for 8h; Inert atmosphere;	98.4%

4-ethylpiperazine (5308-25-8) + 6-Chloro-7,8-dihydro-9-oxa-5-aza-benzo[6,7]cyclohepta[1,2-a]naphthalene (151080-38-5) → 6,7-dihydro-8-(4-ethyl-1-piperazinyl)<1>benzoxepino<4,5-c>quinoline

Conditions	Yield
at 120 - 130℃;	98%

4-ethylpiperazine (5308-25-8) + 6,8-dibromo-1,7-naphthyridine → 6-bromo-8-(4-ethylpiperazin-1-yl)-1,7-naphthyridine (223553-60-4)

Conditions	Yield
at 100℃; for 0.25h; Neat (no solvent);	98%

4-ethylpiperazine (5308-25-8) + formaldehyd (50-00-0) + (E)-7-fluoro-5-(5-(methylthio)-1,3,4-oxadiazol-2-yl)-1H-benzo[e][1,4]diazepin-2(3H)-one (1649449-37-5) → C17H19FN6O2 (1649449-58-0)

Conditions	Yield
In ethanol for 0.183333h; Microwave irradiation;	98%

4-ethylpiperazine (5308-25-8) + 2-fluoropyridine (372-48-5) → 1-(5-bromopyridin-2-yl)-4-ethylpiperazine (364794-57-0)

Conditions	Yield
With potassium carbonate In dimethyl sulfoxide at 120℃; for 2h; Microwave irradiation;	98%

4-ethylpiperazine (5308-25-8) + 7-chloro-1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-3-quinoline carboxylic acid (86393-33-1) → enrofloxacin (93106-60-6)

Conditions	Yield
With nano iron oxide on ZrO2 coated sulfonic acid In water for 0.316667h; Solvent; Temperature; Reagent/catalyst; Reflux;	97%
at 150℃; for 0.416667h; Microwave irradiation;	93%
With aluminum tri-bromide In ethanol at 75℃; for 4h; Reagent/catalyst; Solvent; Temperature;	92%

4-ethylpiperazine (5308-25-8) + 2-(methylthio)-3-nitro-4H-chromen-4-one (1264701-67-8) → 2-(4-ethylpiperazin-1-yl)-3-nitro-4H-chromen-4-one (1264701-87-2)

Conditions	Yield
In 1,4-dioxane Reflux; Combinatorial reaction / High throughput screening (HTS);	97%

4-ethylpiperazine (5308-25-8) + 1-chloro-7-methyl-3-thiophen-2-yl-isoquinoline (1617529-28-8) → 1-(4-ethyl-piperazin-1-yl)-7-methyl-3-thiophen-2-yl-isoquinoline (1617529-21-1)

Conditions	Yield
With potassium carbonate In N,N-dimethyl-formamide at 110℃; Inert atmosphere;	97%

4-ethylpiperazine (5308-25-8) + 3-Chloropyridine (626-60-8) → 1-ethyl-4-(pyridin-3-yl)piperazine

Conditions	Yield
Stage #1: 4-ethylpiperazine With dichloro(3-chloropyridinyl)(1,3-(diisopropylphenyl)-4,5-bis(dimethylamino)imidazol-2-ylidene)palladium(II); potassium tert-butylate for 0.0333333h; Buchwald-Hartwig Coupling; Inert atmosphere; Schlenk technique; Sealed tube; Stage #2: 3-Chloropyridine In 1,2-dimethoxyethane at 25℃; for 18h; Buchwald-Hartwig Coupling; Inert atmosphere; Schlenk technique;	97%

4-ethylpiperazine (5308-25-8) + 1-Phenyl-2-propyn-1-ol (4187-87-5) + 2,2,2-trifluoro-N-(2-iodophenyl)acetamide (143321-89-5) → 2-((4-ethylpiperazin-1-yl)(phenyl)methyl)-1H-indole (1196834-78-2)

Conditions	Yield
With bis-triphenylphosphine-palladium(II) chloride; copper(l) iodide; potassium carbonate In N,N-dimethyl-formamide at 80℃; for 4h; Inert atmosphere;	96%

Upstream product

• 24426-42-4 EtN(CH₂CN)2 
• 60787-02-2 (4-ethylpiperazin-1-yl)(phenyl)methanone 
• 669050-80-0 C₁₁H₂₂N₂O₂ 
• 110-85-0 piperazine 
• 75-00-3 chloroethane 
• 110-72-5 N-ethylethane-1,2-diamine 
• 131543-46-9 Glyoxal 
• 64-17-5 ethanol 
• 156-87-6 propan-1-ol-3-amine 
• 660-68-4 diethyl amine hydrochloride 
• 557-66-4 ethanamine hydrochloride 
• 75-04-7 ethylamine 
• 111-42-2 2,2'-iminobis[ethanol] 
• 821-48-7 bis-(2-chloroethyl)amine hydrochloride 

Downstream Products

• 102019-57-8 (+/-)(1Ξ)-trans-2-[(Ξ)-α-(4-ethyl-piperazino)-benzyl]-cyclohexanol 
• 102019-57-8 (+/-)(1Ξ)-cis-2-[(Ξ)-α-(4-ethyl-piperazino)-benzyl]-cyclohexanol 
• 102009-34-7 1-ethyl-4-(4-chloro-benzhydryl)-piperazine 
• 102019-53-4 1-ethyl-4-(cyclohexyl-phenyl-methyl)-piperazine 
• 103798-48-7 1-(2-acetoxymethyl-2-phenyl-butyryl)-4-ethyl-piperazine 
• 90206-22-7 (4-ethyl-piperazin-1-yl)-acetonitrile 
• 106739-38-2 2-(4-ethyl-piperazino)-1-phenyl-ethanone 
• 48187-94-6 1-(diphenylmethyl)-4-ethylpiperazine 
• 100800-87-1 1-ethyl-4-(4-methoxy-benzenesulfonyl)-piperazine 
• 5048-90-8 1-(hydroxy-diphenyl-acetyl)-4-ethyl-piperazine 
• 110435-59-1 10-<3-(Aethyl-piperazino)-propyl>-phenthiazin. 
• 174358-34-0 PD 163355 
• 186650-78-2 4-(4-ethyl-piperazin-1-yl)-benzonitrile 
• 252233-58-2 5-(4-ethyl-piperazine-1-sulfonyl)-2-propoxy-benzoic acid methyl ester 

Relevant articles and documents

Design and Synthesis of Novel Piperazine (2-Chloroethyl)-1-nitrosourea Analogues as Anticancer Agents

A series of piperazine (2-chloroethyl)-1-nitrosourea analogues (6a-h) have been designed, synthesized, characterized and screened for anticancer activity against five human cancer cell lines viz. human colorectal cancer (HCT-116 and HCT-15), human colon cancer (Colo-205), human breast cancer (MCF-7) and leukaemia (Molt-4). Among the screened compounds, compound 6f exhibits potent activity against HCT-116 cell line with an IC50 of 1.0 μM, which regarded as promising drug candidate for the development of anticancer agents.

Biocatalytic Access to Piperazines from Diamines and Dicarbonyls

Given the widespread importance of piperazines as building blocks for the production of pharmaceuticals, an efficient and selective synthesis is highly desirable. Here we show the direct synthesis of piperazines from 1,2-dicarbonyl and 1,2-diamine substrates using the R-selective imine reductase from Myxococcus stipitatus as biocatalyst. Various N- and C-substituted piperazines with high activity and excellent enantioselectivity were obtained under mild reaction conditions reaching up to 8.1 g per liter.

Characterization of stress degradation products of blonanserin by UPLC-QTOF-tandem mass spectrometry

Stress studies of drugs are very important in the drug development process. As per regulatory guidelines forced degradation studies and characterization of resulting degradation products is mandatory to establish inherent stability of the drug. Blonanserin is an important drug used for the treatment of schizophrenia. As there are no reports in the literature on the degradation study of the drug, the present work has been undertaken. Blonanserin was subjected to forced degradation studies under the conditions of hydrolysis (acidic, basic and neutral), oxidation, photolysis and thermal stress conditions. A selective separation was achieved on a Waters BEH C18 analytical column (50 mm x 2.1 mm, 1.7 μm). The structural characterization of the degradation products was performed using UPLC/QTOF/MS/MS. The drug was found to degrade in oxidative and photolytic conditions, whereas it was stable under hydrolytic, photolytic and thermal stress conditions. A total of seven hitherto unknown degradation products were characterized and probable mechanisms have been proposed for the formation of the degradation products. Moreover, in silico toxicity of all degradation products was also evaluated.