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1-N-Boc-3-hydroxyazetidine

CAS No.
141699-55-0
Chemical Name:
1-N-Boc-3-hydroxyazetidine
Synonyms
TERT-BUTYL 3-HYDROXYAZETIDINE-1-CARBOXYLATE;N-BOC-3-HYDROXYAZETIDINE;Baricitinib-012;JACS-141699-55-0;BUTTPARK 75\04-65;N-Boc-3-Azetidinol;1-Boc-azetidin-3-ol;N-Boc-Azetidin-3-ol;carbamate (ARQ092 RSM2);1-BOC-3-(HYDROXY)AZETIDINE
CBNumber:
CB1428146
Molecular Formula:
C8H15NO3
Molecular Weight:
173.21
MDL Number:
MFCD04115305
MOL File:
141699-55-0.mol
MSDS File:
SDS
TDS File:
TDS
Last updated:2026-04-24 14:58:12
Product description Number Pack Size Price
1-Boc-3-hydroxyazetidine 97% 694347 5g $111
1-Boc-3-hydroxyazetidine 97% 694347 1g $26.2
1-(tert-Butoxycarbonyl)-3-hydroxyazetidine >96.0%(GC) B2922 1g $38
1-(tert-Butoxycarbonyl)-3-hydroxyazetidine >96.0%(GC) B2922 5g $73
1-N-BOC-3-HYDROXYAZETIDINE 97% 56841 25G $18
More product size

1-N-Boc-3-hydroxyazetidine Properties

Melting point 36-43 °C
Boiling point 253.7±33.0 °C(Predicted)
Density 1.184±0.06 g/cm3(Predicted)
Flash point >110℃
storage temp. 2-8°C
solubility soluble in Methanol
form Solid
pka 14.16±0.20(Predicted)
color White to light yellow
InChI InChI=1S/C8H15NO3/c1-8(2,3)12-7(11)9-4-6(10)5-9/h6,10H,4-5H2,1-3H3
InChIKey XRRXRQJQQKMFBC-UHFFFAOYSA-N
SMILES N1(C(OC(C)(C)C)=O)CC(O)C1
CAS DataBase Reference 141699-55-0(CAS DataBase Reference)
UNSPSC Code 12352100
NACRES NA.22

SAFETY

Risk and Safety Statements

Symbol(GHS)  GHS hazard pictogramsGHS hazard pictograms
GHS05,GHS07
Signal word  Danger
Hazard statements  H302-H315-H318-H335
Precautionary statements  P280-P301+P312+P330-P302+P352-P305+P351+P338+P310
target organs Respiratory system
PPE dust mask type N95 (US), Eyeshields, Gloves
Hazard Codes  Xi,Xn
Risk Statements  36/37/38-41-22
Safety Statements  26-36/37/39
WGK Germany  3
TSCA  No
HazardClass  IRRITANT
HS Code  29339900
Storage Class 11 - Combustible Solids
Hazard Classifications Acute Tox. 4 Oral
Eye Dam. 1
Skin Irrit. 2
STOT SE 3
NFPA 704
1
2 0

1-N-Boc-3-hydroxyazetidine price More Price(55)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich 694347 1-Boc-3-hydroxyazetidine 97% 141699-55-0 5g $111 2025-07-31 Buy
Sigma-Aldrich 694347 1-Boc-3-hydroxyazetidine 97% 141699-55-0 1g $26.2 2023-06-20 Buy
TCI Chemical B2922 1-(tert-Butoxycarbonyl)-3-hydroxyazetidine >96.0%(GC) 141699-55-0 1g $38 2026-04-30 Buy
TCI Chemical B2922 1-(tert-Butoxycarbonyl)-3-hydroxyazetidine >96.0%(GC) 141699-55-0 5g $73 2026-04-30 Buy
AstaTech 56841 1-N-BOC-3-HYDROXYAZETIDINE 97% 141699-55-0 25G $18 2026-04-30 Buy
Product number Packaging Price Buy
694347 5g $111 Buy
694347 1g $26.2 Buy
B2922 1g $38 Buy
B2922 5g $73 Buy
56841 25G $18 Buy

1-N-Boc-3-hydroxyazetidine Chemical Properties,Uses,Production

Chemical Properties

white powder

Uses

1-N-Boc-3-hydroxyazetidine is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). 1-N-Boc-3-hydroxyazetidine is also a alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs

Synthesis

1-benzhydrylazetidin-3-Ol

18621-17-5

Di-tert-butyl dicarbonate

24424-99-5

1-N-Boc-3-hydroxyazetidine

141699-55-0

General procedure for the synthesis of N-Boc-3-hydroxyazetidine from 1-diphenylmethyl-3-hydroxyazetidine and di-tert-butyl dicarbonate: (1) Dissolve 1-diphenylmethyl-3-hydroxyazetidine (10.0 g, 41.8 mmol) in methanol (300 ml), add 10% palladium-carbon catalyst (10.0 g), and carry out the catalytic hydrogenation reaction at room temperature for 3 hours. After completion of the reaction, the catalyst was removed by filtration. To the filtrate was added di-tert-butyl dicarbonate (18.2 g, 83.6 mmol) and stirred at room temperature for 1 hour. After completion of the reaction, the reaction mixture was concentrated under reduced pressure. The residue was purified by silica gel column chromatography with the eluent being hexane: ethyl acetate (1:1→1:2) to afford 1-tert-butoxycarbonyl-3-hydroxyazetidine (7.05 g, 97% yield). (2) To a solution of 1-tert-butoxycarbonyl-3-hydroxyazetidine (2.5 g, 14.4 mmol) in dimethylformamide (125 ml) was added sodium hydride (55% oil dispersion) under ice bath conditions. The ice bath was stirred for 10 minutes followed by 30 minutes at room temperature. Subsequently, iodomethane (1.79 ml, 28.8 mmol) was added to the ice bath and the ice bath was stirred for 10 minutes followed by 1 hour at room temperature. After completion of the reaction, 10% aqueous acetic acid solution was added to the ice bath and stirred for 30 minutes. The reaction mixture was partitioned between ethyl acetate and 10% aqueous sodium chloride solution. The organic layer was washed sequentially with saturated aqueous sodium bicarbonate solution and saturated aqueous sodium chloride solution, dried over anhydrous sodium sulfate, filtered and concentrated under reduced pressure. The residue was purified by silica gel column chromatography with hexane:ethyl acetate (2:1) as eluent to afford 1-tert-butoxycarbonyl-3-methoxyazetidine (2.18 g, 81% yield) as a colorless oil.1H-NMR (400 MHz, CDCl3): δ (ppm) 4.16-4.10 (1H, m), 4.09-4.03 (2H, m ), 3.82 (2H, dd, J = 10.2,4.4Hz), 3.28 (3H, s), 1.44 (9H, s).

IC 50

Non-cleavable Linker

References

[1] Beck A, et al. Strategies and challenges for the next generation of antibody-drug conjugates. Nat Rev Drug Discov. 2017;16(5):315-337. DOI:10.1038/nrd.2016.268
[2] Nalawansha DA, et al. PROTACs: An Emerging Therapeutic Modality in Precision Medicine. Cell Chem Biol. 2020;27(8):998-985. DOI:10.7554/eLife.57277

24424-99-5
90604-02-7
141699-55-0
Synthesis of 1-N-Boc-3-hydroxyazetidine from Di-tert-butyl dicarbonate and 1-(Diphenylmethyl)-3-Hydroxyazetidine Hydrochloride
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View Lastest Price from 1-N-Boc-3-hydroxyazetidine manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
1-N-Boc-3-hydroxyazetidine pictures 2025-09-25 1-N-Boc-3-hydroxyazetidine
141699-55-0
US $101.00-1.00 / KG 1KG 99% g-kg-tons, free sample is available Henan Fengda Chemical Co., Ltd
1-N-Boc-3-hydroxyazetidine pictures 2025-04-04 1-N-Boc-3-hydroxyazetidine
141699-55-0
US $0.00-0.00 / KG 1KG 98% 1Ton Henan Aochuang Chemical Co.,Ltd.
1-N-Boc-3-hydroxyazetidine pictures 2024-02-26 1-N-Boc-3-hydroxyazetidine
141699-55-0
US $0.00-0.00 / kg 1kg 98% Kgs BTC Nantong Pharmaceuticals Technology Co.,Ltd

1-N-Boc-3-hydroxyazetidine Spectrum

BUTTPARK 75\04-65 3-HYDROXYAZETIDINE, N-BOC PROTECTED 3-HYDROXY-AZETIDINE-1-CARBOXYLIC ACID TERT-BUTYL ESTER 1-N-BOC-3-HYDROXYAZETIDINE 1-BOC-3-(HYDROXY)AZETIDINE 1-TERT-BUTOXYCARBONYL-3-AZETIDINOL 1-TERT-BUTOXYCARBONYL-3-HYDROXYAZETIDINE 3-Hydroxyazetidine, N-BOC protected 97% 1-tert-Butoxycarbonyl-3-azetidinol tert-butyl 3-hydroxyazetidine-1-carboxylate 1-BOC-3-(HYDROXY)AZETIDINE 1-(tert-Butoxycarbonyl)-3-azetidinol 1-(TERT-BUTOXYCARBONYL)-3-HYDROXYAZETIDINE,98.0%(GC) 1-Boc-azetidin-3-ol 1-Azetidinecarboxylic acid, 3-hydroxy-, 1,1-dimethylethyl ester tert-butyl 3-hydro×yazetidine-1-carbo×ylate 1-Boc-3-hydroxyazetidine tert-Butyl 3-Hydroxyazetidine-1-carboxylate 3-Hydroxyazetidine-1-carboxylic Acid tert-Butyl Ester tert-Butyl 3-hydroxyazetidine-1-carboxylate, 1-(tert-Butoxycarbonyl)-3-hydroxyazetidine 1-Boc-3-(Hydroxy)azetidine ,97% carbamate (ARQ092 RSM2) 3-hydroxy-1-azetidinecarboxylic acid tert-butyl ester 1-Boc-3-hydroxyazetidine 97% N-Boc-Azetidin-3-ol 1-azetidinecarboxylic acid, 3-hydroxy-, 1,1-dimethylethyl JACS-141699-55-0 N-Boc-3-Azetidinol 1-(tert-Butoxycarbonyl)-3-hydroxyazetidine > Baricitinib-012 1-N-Boc-3-hydroxyazetidine ISO 9001:2015 REACH 1-N-Boc-3-hydroxyl-azetidine N-BOC-3-HYDROXYAZETIDINE tert-butyl-3-hydroxyazetidine-4-carboxylate 1-Boc-3-hydroxyazetidine, 95% tert-Butyl 3-hydroxyazetidine-1-carboxylate - [B5483] TERT-BUTYL 3-HYDROXYAZETIDINE-1-CARBOXYLATE 141699-55-0 141699-88-0 41699-55-0 Ring Systems B-Amino Azetidines Simple 4-Membered Ring Compounds CMLLYL