3-Hydroxyazetidine hydrochloride → Methyl 5-fluoro-2-(3-hydroxyazetidin-1-yl)nicotinate

HRID 72435Notes

Reaction equation

HRID 72435 reaction equation
Cl.[NH:2]1[CH2:5][CH:4]([OH:6])[CH2:3]1.Cl[C:8]1[N:17]=[CH:16][C:15]([F:18])=[CH:14][C:9]=1[C:10]([O:12][CH3:13])=[O:11]>>[F:18][C:15]1[CH:16]=[N:17][C:8]([N:2]2[CH2:5][CH:4]([OH:6])[CH2:3]2)=[C:9]([CH:14]=1)[C:10]([O:12][CH3:13])=[O:11]

Participants

3

Reactant 2

HCID 27592903-Hydroxyazetidine hydrochlorideHCID 24229209Methyl 2-chloro-5-fluoronicotinate

Product 1

HCID 67958513Methyl 5-fluoro-2-(3-hydroxyazetidin-1-yl)nicotinate

Procedure

The title compound (D70) (75 mg) was prepared according to the experimental procedure described in Description 62 starting from azetidin-3-ol hydrochloride (208 mg, 1.89 mmol) and methyl 2-chloro-5-fluoronicotinate (300 mg, 1.58 mmol, commercially available from Adesis#2-482).

Sources & evidence

ORD record
ord-9f50c0c70a1044b5ab00b3b845761f4a
Source dataset
uspto-grants-2014_09
Patent number
US08828987B2

Reaction notes

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