2,2-Difluoro-benzo[1,3]dioxole-5-boronic acid synthesis
- Product Name:2,2-Difluoro-benzo[1,3]dioxole-5-boronic acid
- CAS Number:190903-71-0
- Molecular formula:C7H5BF2O4
- Molecular Weight:201.92
33070-32-5
184 suppliers
$6.00/1g
5419-55-6
371 suppliers
$12.00/5g
190903-71-0
82 suppliers
$76.00/100mg
Yield: 100%
Reaction Conditions:
with n-butyllithium in tetrahydrofuran at -65 - -60;Inert atmosphere;
Steps:
8.1 Step 1: Example 8b
Example 8a (15.7 g, 0.066 mol), B(OiPr)3 (18.7 g, 0.099 mol), was dissolved in THF (300 mL), the mixture was cooled to -65°C under N2,n-BuLi (32 mL, 0.079 mol) was added dropwise. After addition,the reaction mixture was stirred at -60°C for lh,then warmed to r.t., NH4C1 (200 mL) and EA (200 mL) was added, the mixture was acidified to pH 2-3 by adding HC1 (3 N). The organic phase was separated, washed with water, brine and dried over Na2S04, filtrated and concentrated under reduced pressure to give the desired product (Example 8b, 16 g, yield 100%) as white solid.
References:
FRONTHERA U.S. PHARMACEUTICALS LLC;JIN, Bohan;DONG, Qing;HUNG, Gene WO2017/218960, 2017, A1 Location in patent:Paragraph 00406
33070-32-5
184 suppliers
$6.00/1g
190903-71-0
82 suppliers
$76.00/100mg