China New Product R-2-(Methoxymethyl)pyrrolidine - (R)-(-)-3-Pyrrolidinol Hydrochloride CAS 104706-47-0 Purity ≥99.7% (GC) Chiral Purity ≥99.7% Panipenem and Darifenacin hydrobromide Intermediate – Ruifu

Manufacturer Supply; High Purity and Competitive Price
Shanghai Ruifu Chemical Co., Ltd. Commercial Supply Chiral Compounds:
(R)-(-)-3-Pyrrolidinol Hydrochloride CAS: 104706-47-0
(S)-3-Hydroxypyrrolidine hydrochloride CAS: 122536-94-1
Intermediate of Panipenem (CAS 87726-17-8) and Darifenacin hydrobromide (CAS 133099-07-7)

Package: Bottle, Aluminum foil bag, Cardboard drum, 25kg/Drum, or according to customer’s requirement.

Storage Condition: Store in sealed containers at cool and dry place; Protect from light, moisture and pest infestation.

Manufacturer Supply; High Purity and Competitive Price
Shanghai Ruifu Chemical Co., Ltd. Commercial Supply Chiral Compounds:
(R)-(-)-3-Pyrrolidinol Hydrochloride CAS: 104706-47-0
(S)-(+)-3-Hydroxypyrrolidine hydrochloride CAS: 122536-94-1
Intermediate of Panipenem (CAS 87726-17-8) and Darifenacin hydrobromide (CAS 133099-07-7)

Darifenacin, an orally active, once a day selective M3 receptor antagonist, was launched for the treatment of overactive bladder in patients with symptoms of urge urinary incontinence, urgency and frequency. The drug selectively inhibits M3 receptor in the detrusor muscle while sparing the M1 and M2 receptors that are believed to be involved in central nervous system and cardiovascular function respectively. The compound was originally developed by Pfizer and licensed to Novartis and Bayer.

Route of Synthesis of (R)-3-Hydroxypyrrolidine hydrochloride
(R) -4-chloro-3-hydroxybutanitrile was reacted with trimethyl chlorosilane in dichloromethane solvent to obtain (R) -4-chloro-3-trimethylsiloxy butanitrile.(R) -4-chloro-3-trimethylsiloxyebutylamine was then hydrogenated on Pd/C catalyst.(R) -3-trimethylsiloxyepyrrolidine was obtained by sodium hydroxide ring closing treatment.Finally, the (R) -3-hydroxypyrrolidine hydrochloride product was obtained by concentrated hydrochloric acid treatment and the trimethylsilyl protective group was removed.

Analysis Method
Eqiupment: GC instrument (Shimadzu GC-2010)
Column: DB-17 Agilent 30mX0.53mmX1.0μm
Initial oven temperature:      80℃
Initial time                             2.0min
Rate                                     15℃/min
Final oven temperature:       250℃
Final time                             20min
Carrier gas                           Nitrogen
Mode                                    Constant flow
Flow                                     5.0mL/min
Split ratio                              10:1
Injector temperature:            250℃
Detector temperature:          300℃
Injection volume                    1.0μL

Precautions to be taken before analysis:
1. Condition column at 240℃ for minimum 30minutes.
2. Wash the syringe and clean injector liner properly to remove the contaminants of earlier analysis.
3. Wash, dry and fill diluent in syringe wash vials.
Diluent preparation:
Prepare 2% w/v sodium hydroxide solution in water.
Standard preparation:
Weigh about 100mg of (R)-3-hydroxyprrolidine hydrochloride standard into a vial, add 1mL of diluent and dissolve.
Test preparation:
Weigh about 100mg of test sample into a vial, add 1mL of diluent and dissolve. Prepare in duplicate.
Procedure:
Inject blank (diluent), standard preparation and test preparation using above GC conditions. Disregard the peaks due to blank. The retention time of peak due to (R)-3-hydroxyprrolidine is about 5.0min.
Note:
Report the result as an average