DayangChem exported this product to many countries and regions at best price. If you are looking for the material's manufacturer or supplier in China, DayangChem is your best choice. Pls contact with us freely for getting detailed product spe
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inquiryOur main production base is located in Xuzhou industry park. We are certified both to the ISO 9001 and ISO 14001 Standards, have a safety management system in place.Our R&D team masters core technology for process-design of target building block
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inquiryProduct Name: (1S,4S)-2-BOC-2,5-DIAZABICYCLO[2.2.1]HEPTANE Synonyms: TERT-BUTYL (1S, 4S)-(-)-2,5-DIAZABICYCLO[2.2.1]HEPTANE-2-CARBOXYLATE;TERT-BUTYL (1S,4S)-2,5-DIAZABICYCLO(2.2.1)HEPTANE-2-CARBOXYLATE;1,1-DIMETHYLETHYL (1S,4S)-2,5-DIA
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inquiryOur Advantage Rich Experience Our products are sold all over Europe,North&South America, Sino-East, Asia and pacific area as well as Africa,we establish long term. Quality service Company cooperates with research institutes. We strictly con
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inquiryWITH US,YOUR MONEY IN SAFE,YOUR BUSINESS IN SAFE 1)Quick Response Within 12 hours; 2)Quality Guarantee: All products are strictly tested by our QC, confirmed by QA and approved by third party lab in China, USA, Canada, Germany, UK, Italy, France et
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inquiry(1S,4S)-2-BOC-2,5-DIAZABICYCLO[2.2.1]HEPTANE CAS:113451-59-5 Qingdao Belugas Import and Export Co., Ltd. is a scientific and technological company integrating research and development, production and trade of chemical intermediates, specializing in
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inquiryHenan Wentao Chemical Product Co.,Ltd is Located in Zhengzhou High-tech Development Zone with import and export license, We passed ISO 9001:2008 as well, Henan Wentao has developed more than 1000 compounds, which are widely used in the fields of prod
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inquiryA substitute for perfluorooctanoic acid, mainly used as a surfactant, dispersant, additive, etc Appearance:White solid or Colorless liquid Purity:99.3 % We will ship the goods in a timely manner as required We can provide relevant documents acc
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inquiryJ&H CHEM R&D center can offer custom synthesis according to the contract research and development services for the fine chemicals, pharmaceutical, biotechnique and some of the other chemicals. J&H CHEM has some Manufacturing base in Jia
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inquiryZibo Hangyu Biotechnology Development Co., Ltd is a leading manufacturer and supplier of chemicals in China. We develop produce and distribute high quality pharmaceuticals, intermediates, special chemicals and OLED intermediates and other fine chemi
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inquiryThe above product is Ality Chemical's strong item with best price, good quality and fast supply. Ality Chemical has been focusing on the research and production of this field for over 14 years. At the same time, we are always committed to providing h
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inquiryGMP standard, high purity, competitive price, in stock 1. Quick Response: within 6 hours after receiving your email. 2. Quality Guarantee: All products are strictly tested by our QC, confirmed by QA, and approved by a third-party lab in China, USA,
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inquiryProduct Name: (1S,4S)-2-BOC-2,5-DIAZABICYCLO[2.2.1]HEPTANE Synonyms: TERT-BUTYL (1S, 4S)-(-)-2,5-DIAZABICYCLO[2.2.1]HEPTANE-2-CARBOXYLATE;TERT-BUTYL (1S,4S)-2,5-DIAZABICYCLO(2.2.1)HEPTANE-2-CARBOXYLATE;(1S,4S)-N-(TERT-BUTOXYCARBONYL)-2,5-DIAZAB
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inquiryWe Huarong Pharm can provide Customized Synthesis & Process R&D & APIs and intermediates Production & Quality Research & Registration Application, especially our GMP validation service which complies with SFDA, FDA, WHO and EU EMPA. O
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inquiryGOLDEN PHARMA CO.,LIMITED.is a professional pharmaceutical company,our team have more than 20years expereince in pharmaceutical production and sales. we are a professional technical enterprise specializing in the R & D, production,QA regulation
Cas:113451-59-5
Min.Order:1 Kilogram
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inquiryShanghai Finebiotech Co.,Ltd.was established in 2020, which providing professional chemical services. As a customer-oriented company, we have distinguished ourself from others in providing worldwide customers with cost-effective and efficient service
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inquiryStock products, own laboratory Package:Grams, Kilograms Application:For R&D Transportation:According to customer request Port:Shanghai
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inquiryLower price, sample is available,SDS test documents are available,large stock in warehouseAppearance:White powder Storage:Sealed and preserved Package:200/Kilograms Application:Fine chemical intermediates, used as the main raw material for the synthe
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inquiryhigh purity lowest priceAppearance:solid or liquid Storage:in sealed air resistant place Package:drum and bag Application:for pharma use Transportation:by sea or air Port:Beijing or Guangzhou
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inquiryhigh quality Storage:Sealed, dry, microtherm , avoid light and smell. Package:According to the demand of customer Application:Organic synthesis Transportation:by air or by sea
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inquiryhigh purity lowest priceAppearance:solid or liquid Storage:in sealed air resistant place Package:Foil bag; Drum; Plastic bottle Application:Pharma;Industry;Agricultural Transportation:by sea or air Port:Beijing or Guangzhou
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inquiryHunan chemfish Pharmaceutical co.,Ltd.located in Lugu High-tech industral park ,Hunan province . with its own R&D center and more than 10000㎡manufacture plant . Chemfish owns 40 reactors from 1000L to 8000L. With complete auxiliary equipment as
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inquiryAnsciep Chemical is a professional enterprise manufacturing and distributing fine chemicals and speciality chemicals. We have been dedicated to heterocycle compounds and phenyl rings for tens of years. This is our mature product for export. Our quali
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inquirystocks,competitive price,superior product If you nee, pls feel free to contact me. Storage:Preserve In Well-Closed, Light-Resistant and Tight Containers. Store In Cool & Dry Place Package:1g,5g,10g...1kg,5kg...more Application:R&D Transportation:sh
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Min.Order:1 Gram
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inquiryWe product this chemical more than 10 years . We are very experience to export it to many countries, Our superior & stable quality , competitive price gain warm reception from our customers. Application:Chemical intermediate
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inquiryAppearance:solid or liquid Storage:sealed in cool and dry place Package:As customer's requested Application:Pharma Intermediate Transportation:by courier/air/sea Port:Any port in China
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inquirytert-Butyl (1S,4S)-2,5-diazabicyclo[2.2.1]heptan-2-carboxylate cas 113451-59-5Appearance:white crystalline powder Storage:Store in dry, dark and ventilated place Package:25KG drum Application:intermediate Transportation:by air, by sea, by express
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inquiry113451-59-5 Application:intermediate
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inquirylow price and high purityAppearance:solid or liquid Storage:in sealed air resistant place Package:As customer require Application:Pharma;Industry;Agricultural Transportation:by sea or by airplane Port:any port in China
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inquiryR & D enterprises have their own stock in stockAppearance:To be subject to the object Package:Customized Application:pharmaceutical intermediates Transportation:Air Port:Shanghai;Guangzhou
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inquiry(2S,4R)-2-(azidomethyl)-1-(tert-butoxycarbonyl)-4-<(methylsulfonyl)oxy>pyrrolidine
(1S,4S)-2,5-Diaza-bicyclo[2.2.1]heptane-2-carboxylic acid tert-butyl ester
Conditions | Yield |
---|---|
With hydrogen; palladium on activated charcoal In methanol | 100% |
Stage #1: (2S,4R)-2-(azidomethyl)-1-(tert-butoxycarbonyl)-4-<(methylsulfonyl)oxy>pyrrolidine With triphenylphosphine In tetrahydrofuran at 20℃; for 2h; Staudinger Azide Reduction; Stage #2: With water In tetrahydrofuran for 18h; | 71% |
(1S,4S)-5-Benzyl-2-tert-butoxycarbonyl-2,5-diazabicyclo<2.2.1>heptane
(1S,4S)-2,5-Diaza-bicyclo[2.2.1]heptane-2-carboxylic acid tert-butyl ester
Conditions | Yield |
---|---|
With palladium hydroxide 10 wt. % on activated carbon; hydrogen In methanol under 3102.97 Torr; | 90% |
With palladium 10% on activated carbon; hydrogen In methanol at 50℃; under 22502.3 Torr; for 16h; | 85% |
With 10% palladium on carbon; hydrogen | 76% |
With palladium 10% on activated carbon; hydrogen In dichloromethane under 3102.97 Torr; | 10.4 g |
tert-butyl (2S,4S)-4-amino-2-(hydroxymethyl)pyrrolidin-1-carboxylate
(1S,4S)-2,5-Diaza-bicyclo[2.2.1]heptane-2-carboxylic acid tert-butyl ester
Conditions | Yield |
---|---|
With di-isopropyl azodicarboxylate; triphenylphosphine In tetrahydrofuran at 22 - 25℃; for 12h; Inert atmosphere; | 80.6% |
L-4-hydroxyproline methyl ester hydrochloride
(1S,4S)-2,5-Diaza-bicyclo[2.2.1]heptane-2-carboxylic acid tert-butyl ester
Conditions | Yield |
---|---|
Multi-step reaction with 6 steps 1.1: triethylamine / dichloromethane / 17 h / 0 °C 2.1: lithium borohydride / tetrahydrofuran / 26 h / 0 - 20 °C 3.1: pyridine / dichloromethane / 18 h / 40 °C 4.1: trimethylsilylazide; tetrabutyl ammonium fluoride / tetrahydrofuran / 18 h / 70 °C 5.1: triethylamine / dichloromethane / 0.5 h / 0 °C 6.1: triphenylphosphine / tetrahydrofuran / 2 h / 20 °C 6.2: 18 h View Scheme |
4R-4-hydroxyproline
(1S,4S)-2,5-Diaza-bicyclo[2.2.1]heptane-2-carboxylic acid tert-butyl ester
Conditions | Yield |
---|---|
Multi-step reaction with 7 steps 1.1: thionyl chloride; hydrogenchloride / water / 18 h / 20 °C / Reflux 2.1: triethylamine / dichloromethane / 17 h / 0 °C 3.1: lithium borohydride / tetrahydrofuran / 26 h / 0 - 20 °C 4.1: pyridine / dichloromethane / 18 h / 40 °C 5.1: trimethylsilylazide; tetrabutyl ammonium fluoride / tetrahydrofuran / 18 h / 70 °C 6.1: triethylamine / dichloromethane / 0.5 h / 0 °C 7.1: triphenylphosphine / tetrahydrofuran / 2 h / 20 °C 7.2: 18 h View Scheme | |
Multi-step reaction with 6 steps 1.1: sodium carbonate / water 1.3: 20 h 2.1: toluene / Reflux 3.1: hydrogen bromide 4.1: sodium methylate / methanol / 20 °C 5.1: triethylamine / dichloromethane / 0 - 20 °C 6.1: hydrogen; palladium hydroxide 10 wt. % on activated carbon / methanol / 3102.97 Torr View Scheme |
1-tert-butyl 2-methyl (2S,4R)-4-hydroxy-1,2-pyrrolidinedicarboxylate
(1S,4S)-2,5-Diaza-bicyclo[2.2.1]heptane-2-carboxylic acid tert-butyl ester
Conditions | Yield |
---|---|
Multi-step reaction with 5 steps 1.1: lithium borohydride / tetrahydrofuran / 26 h / 0 - 20 °C 2.1: pyridine / dichloromethane / 18 h / 40 °C 3.1: trimethylsilylazide; tetrabutyl ammonium fluoride / tetrahydrofuran / 18 h / 70 °C 4.1: triethylamine / dichloromethane / 0.5 h / 0 °C 5.1: triphenylphosphine / tetrahydrofuran / 2 h / 20 °C 5.2: 18 h View Scheme | |
Multi-step reaction with 4 steps 1: triethylamine / dichloromethane / 2 h / 5 - 25 °C 2: sodium azide / N,N-dimethyl-formamide / 3 h / 90 °C 3: potassium borohydride; lithium chloride / tetrahydrofuran / 12 h / 25 °C 4: triphenylphosphine; di-isopropyl azodicarboxylate / tetrahydrofuran / 12 h / 22 - 25 °C / Inert atmosphere View Scheme | |
Multi-step reaction with 4 steps 1: sodium tetrahydroborate / methanol / 18 h / 20 - 35 °C / Cooling with ice; Large scale 2: triethylamine / dichloromethane / 1 h / 20 - 35 °C / Cooling with liquid nitrogen; Large scale 3: 3 h / 80 °C / Large scale 4: palladium 10% on activated carbon; hydrogen / methanol / 16 h / 50 °C / 22502.3 Torr View Scheme |
tert-butyl (2S,4R)-4-hydroxy-2-hydroxymethyl-pyrrolidine-1-carboxylate
(1S,4S)-2,5-Diaza-bicyclo[2.2.1]heptane-2-carboxylic acid tert-butyl ester
Conditions | Yield |
---|---|
Multi-step reaction with 4 steps 1.1: pyridine / dichloromethane / 18 h / 40 °C 2.1: trimethylsilylazide; tetrabutyl ammonium fluoride / tetrahydrofuran / 18 h / 70 °C 3.1: triethylamine / dichloromethane / 0.5 h / 0 °C 4.1: triphenylphosphine / tetrahydrofuran / 2 h / 20 °C 4.2: 18 h View Scheme | |
Multi-step reaction with 3 steps 1: triethylamine / dichloromethane / 1 h / 20 - 35 °C / Cooling with liquid nitrogen; Large scale 2: 3 h / 80 °C / Large scale 3: palladium 10% on activated carbon; hydrogen / methanol / 16 h / 50 °C / 22502.3 Torr View Scheme |
tert-butyl (2S,4R)-4-hydroxy-2-({[(4-methylphenyl)sulfonyl]oxy}methyl)-pyrrolidine-1-carboxylate
(1S,4S)-2,5-Diaza-bicyclo[2.2.1]heptane-2-carboxylic acid tert-butyl ester
Conditions | Yield |
---|---|
Multi-step reaction with 3 steps 1.1: trimethylsilylazide; tetrabutyl ammonium fluoride / tetrahydrofuran / 18 h / 70 °C 2.1: triethylamine / dichloromethane / 0.5 h / 0 °C 3.1: triphenylphosphine / tetrahydrofuran / 2 h / 20 °C 3.2: 18 h View Scheme |
(2S,4R)-tert-butyl 2-(azidomethyl)-4-hydroxypyrrolidine-1-carboxylate
(1S,4S)-2,5-Diaza-bicyclo[2.2.1]heptane-2-carboxylic acid tert-butyl ester
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1.1: triethylamine / dichloromethane / 0.5 h / 0 °C 2.1: triphenylphosphine / tetrahydrofuran / 2 h / 20 °C 2.2: 18 h View Scheme |
N-tert-butoxycarbonyl-cis-4-azido-L-proline methyl ester
(1S,4S)-2,5-Diaza-bicyclo[2.2.1]heptane-2-carboxylic acid tert-butyl ester
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1: potassium borohydride; lithium chloride / tetrahydrofuran / 12 h / 25 °C 2: triphenylphosphine; di-isopropyl azodicarboxylate / tetrahydrofuran / 12 h / 22 - 25 °C / Inert atmosphere View Scheme |
(2S,4R)-4-(methylsulfonyloxy)pyrrolidine-1,2-dicarboxylic acid 1-tert-butylester-2-methylester
(1S,4S)-2,5-Diaza-bicyclo[2.2.1]heptane-2-carboxylic acid tert-butyl ester
Conditions | Yield |
---|---|
Multi-step reaction with 3 steps 1: sodium azide / N,N-dimethyl-formamide / 3 h / 90 °C 2: potassium borohydride; lithium chloride / tetrahydrofuran / 12 h / 25 °C 3: triphenylphosphine; di-isopropyl azodicarboxylate / tetrahydrofuran / 12 h / 22 - 25 °C / Inert atmosphere View Scheme |
(2S,4R)-1-(4-tolylsulfonyl)-4-<(4-tolylsulfonyl)oxy>-2-<<(4-tolylsulfonyl)oxy>methyl>pyrrolidine
(1S,4S)-2,5-Diaza-bicyclo[2.2.1]heptane-2-carboxylic acid tert-butyl ester
Conditions | Yield |
---|---|
Multi-step reaction with 5 steps 1: toluene / Reflux 2: hydrogen bromide 3: sodium methylate / methanol / 20 °C 4: triethylamine / dichloromethane / 0 - 20 °C 5: hydrogen; palladium hydroxide 10 wt. % on activated carbon / methanol / 3102.97 Torr View Scheme |
(1S,4S)-5-Benzyl-2-tosyl-2,5-diazabicyclo<2.2.1>heptane
(1S,4S)-2,5-Diaza-bicyclo[2.2.1]heptane-2-carboxylic acid tert-butyl ester
Conditions | Yield |
---|---|
Multi-step reaction with 4 steps 1: hydrogen bromide 2: sodium methylate / methanol / 20 °C 3: triethylamine / dichloromethane / 0 - 20 °C 4: hydrogen; palladium hydroxide 10 wt. % on activated carbon / methanol / 3102.97 Torr View Scheme |
(1S,4S)-2-Benzyl-2,5-diazabicyclo<2.2.1>heptane dihydrobromide
(1S,4S)-2,5-Diaza-bicyclo[2.2.1]heptane-2-carboxylic acid tert-butyl ester
Conditions | Yield |
---|---|
Multi-step reaction with 3 steps 1: sodium methylate / methanol / 20 °C 2: triethylamine / dichloromethane / 0 - 20 °C 3: hydrogen; palladium hydroxide 10 wt. % on activated carbon / methanol / 3102.97 Torr View Scheme | |
Multi-step reaction with 3 steps 1: sodium methylate / methanol / 20 °C 2: triethylamine / dichloromethane / 0 - 20 °C 3: palladium 10% on activated carbon; hydrogen / dichloromethane / 3102.97 Torr View Scheme |
(1S,4S)-N-Benzyl-2,5-diazabicyclo-[2.2.1]heptane
(1S,4S)-2,5-Diaza-bicyclo[2.2.1]heptane-2-carboxylic acid tert-butyl ester
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1: triethylamine / dichloromethane / 0 - 20 °C 2: hydrogen; palladium hydroxide 10 wt. % on activated carbon / methanol / 3102.97 Torr View Scheme | |
Multi-step reaction with 2 steps 1: triethylamine / dichloromethane / 0 - 20 °C 2: palladium 10% on activated carbon; hydrogen / dichloromethane / 3102.97 Torr View Scheme |
2-(2-ethylbenzoimidazol-1-yl)-9-methyl-6-morpholin-4-yl-9H-purine-8-carbaldehyde
(1S,4S)-2,5-Diaza-bicyclo[2.2.1]heptane-2-carboxylic acid tert-butyl ester
C30H39N9O3
Conditions | Yield |
---|---|
Stage #1: 2-(2-ethylbenzoimidazol-1-yl)-9-methyl-6-morpholin-4-yl-9H-purine-8-carbaldehyde; (1S,4S)-2,5-Diaza-bicyclo[2.2.1]heptane-2-carboxylic acid tert-butyl ester In 1,2-dichloro-ethane at 20℃; for 3h; Molecular sieve; Stage #2: With sodium tris(acetoxy)borohydride In 1,2-dichloro-ethane at 20℃; for 17h; Molecular sieve; | 100% |
(1S,4S)-2,5-Diaza-bicyclo[2.2.1]heptane-2-carboxylic acid tert-butyl ester
(1S,4S)-2,5-Diazabicyclo<2.2.1>heptane dihydrochloride
Conditions | Yield |
---|---|
With hydrogenchloride In 1,4-dioxane; methanol at 20℃; for 0.5h; | 100% |
methanesulfonyl chloride
(1S,4S)-2,5-Diaza-bicyclo[2.2.1]heptane-2-carboxylic acid tert-butyl ester
Conditions | Yield |
---|---|
With triethylamine In tetrahydrofuran at 0 - 20℃; for 20h; | 100% |
With triethylamine In tetrahydrofuran at 0 - 30℃; for 12h; Inert atmosphere; | 100% |
isobutyryl chloride
(1S,4S)-2,5-Diaza-bicyclo[2.2.1]heptane-2-carboxylic acid tert-butyl ester
Conditions | Yield |
---|---|
With triethylamine In dichloromethane at 20℃; Inert atmosphere; | 100% |
5-bromopyrimidine
(1S,4S)-2,5-Diaza-bicyclo[2.2.1]heptane-2-carboxylic acid tert-butyl ester
Conditions | Yield |
---|---|
99% | |
With sodium t-butanolate; tris-(dibenzylideneacetone)dipalladium(0); 2,2'-bis-(diphenylphosphino)-1,1'-binaphthyl In toluene at 80 - 85℃; for 5h; | 91% |
With tris-(dibenzylideneacetone)dipalladium(0); sodium t-butanolate In toluene at 80 - 85℃; for 5h; | 91% |
3-Bromopyridine
(1S,4S)-2,5-Diaza-bicyclo[2.2.1]heptane-2-carboxylic acid tert-butyl ester
(1S,4S)-tert-butyl 5-(pyridin-3-yl)-2,5-diazabicyclo[2.2.1]heptane-2-carboxylate
Conditions | Yield |
---|---|
99% | |
With tris-(dibenzylideneacetone)dipalladium(0); 2,2'-bis-(diphenylphosphino)-1,1'-binaphthyl; sodium t-butanolate In toluene at 85℃; for 64h; Inert atmosphere; | 99% |
With sodium t-butanolate; tris-(dibenzylideneacetone)dipalladium(0); 2,2'-bis-(diphenylphosphino)-1,1'-binaphthyl In toluene at 80 - 85℃; for 5h; |
2,5 dichloropyridine
(1S,4S)-2,5-Diaza-bicyclo[2.2.1]heptane-2-carboxylic acid tert-butyl ester
Conditions | Yield |
---|---|
99% |
ethyl 6-chloro-5-cyano-2-methylnicotinate
(1S,4S)-2,5-Diaza-bicyclo[2.2.1]heptane-2-carboxylic acid tert-butyl ester
(1S,4S)-tert-butyl 5-(3-cyano-5-(ethoxycarbonyl)-6-methylpyridin-2-yl)-2,5-diazabicyclo[2.2.1]heptane-2-carboxylate
Conditions | Yield |
---|---|
With N-ethyl-N,N-diisopropylamine In N,N-dimethyl-formamide at 20℃; for 1h; | 99% |
With N-ethyl-N,N-diisopropylamine In N,N-dimethyl-formamide at 20℃; for 1h; | 99% |
4-tert-butylbenzenesulfonyl chloride
(1S,4S)-2,5-Diaza-bicyclo[2.2.1]heptane-2-carboxylic acid tert-butyl ester
C20H30N2O4S
Conditions | Yield |
---|---|
With N-ethyl-N,N-diisopropylamine In dichloromethane at 20℃; for 48h; | 99% |
With N-ethyl-N,N-diisopropylamine In dichloromethane | |
With N-ethyl-N,N-diisopropylamine In dichloromethane at 20℃; for 16h; Inert atmosphere; |
1-iodo-2-diphenylmethoxy-ethane
(1S,4S)-2,5-Diaza-bicyclo[2.2.1]heptane-2-carboxylic acid tert-butyl ester
(1S,4S)-2-[2-(diphenylmethoxy)ethyl]-5-t-Boc-2,5-diazabicyclo[2.2.1]heptane
Conditions | Yield |
---|---|
With potassium carbonate In tetrahydrofuran Heating; | 98% |
(1S,4S)-2,5-Diaza-bicyclo[2.2.1]heptane-2-carboxylic acid tert-butyl ester
Conditions | Yield |
---|---|
With N-ethyl-N,N-diisopropylamine In 1-methyl-pyrrolidin-2-one at 50℃; | 98% |
bromobenzene
(1S,4S)-2,5-Diaza-bicyclo[2.2.1]heptane-2-carboxylic acid tert-butyl ester
Conditions | Yield |
---|---|
With sodium t-butanolate; tris-(dibenzylideneacetone)dipalladium(0); 2,2'-bis-(diphenylphosphino)-1,1'-binaphthyl In toluene at 80 - 85℃; for 5h; | 97% |
1-(3-methoxy-4 nitrophenyl)piperidin-4-one
(1S,4S)-2,5-Diaza-bicyclo[2.2.1]heptane-2-carboxylic acid tert-butyl ester
1,1-dimethylethyl (1S,4S)-5-{1-[3-(methyloxy)-4-nitrophenyl]-4-piperidinyl}-2,5-diazabicyclo[2.2.1]heptane-2-carboxylate
Conditions | Yield |
---|---|
Stage #1: 1-(3-methoxy-4 nitrophenyl)piperidin-4-one; (1S,4S)-2,5-Diaza-bicyclo[2.2.1]heptane-2-carboxylic acid tert-butyl ester With sodium tris(acetoxy)borohydride; acetic acid; triethylamine In dichloromethane for 1h; Stage #2: With sodium hydrogencarbonate In dichloromethane; water | 96% |
(1S,4S)-2,5-Diaza-bicyclo[2.2.1]heptane-2-carboxylic acid tert-butyl ester
Acetoxyacetyl chloride
5-(2-acetoxy-acetyl)-2,5-diaza-bicyclo[2.2.1]heptane-2-carboxylic acid tert-butyl ester
Conditions | Yield |
---|---|
Stage #1: (1S,4S)-2,5-Diaza-bicyclo[2.2.1]heptane-2-carboxylic acid tert-butyl ester With triethylamine In dichloromethane at 5℃; for 0.833333h; Stage #2: Acetoxyacetyl chloride In dichloromethane for 16h; | 96% |
1-(2,4,6-trifluorophenyl)ethan-1-one
(1S,4S)-2,5-Diaza-bicyclo[2.2.1]heptane-2-carboxylic acid tert-butyl ester
tert-butyl (1S,4S)-5-(2-acetyl-3,5-difluorophenyl)-2,5-diazabicyclo[2.2.1]heptane-2-carboxylate
Conditions | Yield |
---|---|
With potassium carbonate In 1,4-dioxane at 100℃; for 24h; Inert atmosphere; regioselective reaction; | 96% |
(1S,4S)-4-(2,5-dimethyl-1H-pyrrol-1-yl)-1-isopropylcyclopent-2-ene-1-carboxylic acid
(1S,4S)-2,5-Diaza-bicyclo[2.2.1]heptane-2-carboxylic acid tert-butyl ester
C25H37N3O3
Conditions | Yield |
---|---|
With O-(benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium tetrafluoroborate; triethylamine In N,N-dimethyl-formamide at 0℃; | 95% |
4-chloromethylbenzaldehyde
(1S,4S)-2,5-Diaza-bicyclo[2.2.1]heptane-2-carboxylic acid tert-butyl ester
Conditions | Yield |
---|---|
With potassium carbonate In acetonitrile at 50℃; | 93.1% |
(1S,4S)-2,5-Diaza-bicyclo[2.2.1]heptane-2-carboxylic acid tert-butyl ester
trifluoroacetic anhydride
(1S,4S)-5-(2,2,2-trifluoroacetyl)-2,5-diazabicyclo[2.2.1]heptane-2-carboxylic acid tert-butyl ester
Conditions | Yield |
---|---|
With triethylamine In tetrahydrofuran at 0℃; for 5h; Inert atmosphere; | 93% |
With triethylamine In tetrahydrofuran at 20℃; for 1h; |
(1S,4S)-2,5-Diaza-bicyclo[2.2.1]heptane-2-carboxylic acid tert-butyl ester
Conditions | Yield |
---|---|
With potassium carbonate In acetonitrile at 80℃; for 24h; | 93% |
With potassium carbonate In acetonitrile at 80℃; for 24h; | 93% |
N-(Benzyloxycarbonyl)glycine
(1S,4S)-2,5-Diaza-bicyclo[2.2.1]heptane-2-carboxylic acid tert-butyl ester
1,1-dimethylethyl(1S,4S)-5-(N-{[benzyloxy]carbonyl}glycyl)-2,5-diazabicyclo[2.2.1]heptane-2-carboxylate
Conditions | Yield |
---|---|
With 3-methyl-N-(3-methylbutyl)-1-butanamine; benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride In dichloromethane at 20℃; | 92% |
With 4-methyl-morpholine; benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride In dichloromethane | |
With 4-methyl-morpholine; benzotriazol-1-ol; N-(3-dimethylaminopropyl)-N-ethylcarbodiimide In dichloromethane at 20℃; for 24h; Product distribution / selectivity; |
2-[4-(2-bromoethoxy)phenoxy]benzothiazole
(1S,4S)-2,5-Diaza-bicyclo[2.2.1]heptane-2-carboxylic acid tert-butyl ester
(S,S)-5-(2-[4-(benzothiazol-2-yloxy)-phenoxy]-ethyl)-2,5-diaza-bicyclo[2.2.1]heptane-2-carboxylic acid tert-butyl ester
Conditions | Yield |
---|---|
With N-ethyl-N,N-diisopropylamine In acetonitrile at 20 - 60℃; for 69h; | 92% |
(1S,4S)-2,5-Diaza-bicyclo[2.2.1]heptane-2-carboxylic acid tert-butyl ester
Conditions | Yield |
---|---|
With nitrogen(II) oxide; calcium hydroxide In water at 20℃; under 12929 Torr; for 120h; Green chemistry; | 92% |
(1S,4S)-2,5-Diaza-bicyclo[2.2.1]heptane-2-carboxylic acid tert-butyl ester
2-[bis(4-fluorophenyl)methoxy]ethyl iodide
3-[2-[bis(4-fluorophenyl)methoxy]ethyl]-8-(1S,4S)-N-t-Boc-2,5-diazabicyclo[2.2.1]heptane
Conditions | Yield |
---|---|
With potassium carbonate In tetrahydrofuran Heating; | 91% |
(1S,4S)-2,5-Diaza-bicyclo[2.2.1]heptane-2-carboxylic acid tert-butyl ester
Conditions | Yield |
---|---|
With N-ethyl-N,N-diisopropylamine In dimethyl sulfoxide at 90℃; | 90% |
6-methoxy-3-pyridinecarboxaldehyde
(1S,4S)-2,5-Diaza-bicyclo[2.2.1]heptane-2-carboxylic acid tert-butyl ester
Conditions | Yield |
---|---|
With sodium tris(acetoxy)borohydride In 1,2-dichloro-ethane at 20℃; | 90% |
2-fluoro-5-nitrobenzaldehye
(1S,4S)-2,5-Diaza-bicyclo[2.2.1]heptane-2-carboxylic acid tert-butyl ester
Conditions | Yield |
---|---|
With potassium carbonate In N,N-dimethyl-formamide at 50℃; Inert atmosphere; | 89% |
Fmoc-Leu-OH
(1S,4S)-2,5-Diaza-bicyclo[2.2.1]heptane-2-carboxylic acid tert-butyl ester
1,1-dimethylethyl (1S,4S)-5-(N-{[(9H-fluoren-9-ylmethyl)oxy]carbonyl}-L-leucyl)-2,5-diazabicyclo[2.2.1]heptane-2-carboxylate
Conditions | Yield |
---|---|
With 4-methyl-morpholine; benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride In dichloromethane at 20℃; | 88.3% |
(1S,4S)-2,5-Diaza-bicyclo[2.2.1]heptane-2-carboxylic acid tert-butyl ester
Conditions | Yield |
---|---|
With potassium carbonate In acetonitrile at 80℃; for 12h; | 87.7% |
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