1. Product Overview & Specifications

2. Key Applications & Use Cases

Pharmaceutical Development

• MAGL Inhibitor Synthesis: Core building block for monoacylglycerol lipase inhibitors with CNS activity
• PROTAC Linkers: Enables construction of E3 ligase-recruiting molecules via hydroxyl group conjugation
• ADC Payloads: Hydroxyl site permits controlled drug-antibody conjugation

Chemical Synthesis

• Selective Protection: Boc group enables orthogonal protection strategies in multi-step syntheses
• Chiral Resolution: (R)-configuration critical for enantioselective catalysis applications
• Ring Modification: Base structure for creating fused heterocyclic systems

3. Practical Case Studies

Case 1: Neuropathic Pain Treatment Development

Challenge: Improve metabolic stability of MAGL inhibitor candidates
Solution: Used (R)-1-Boc-3-Hydroxypiperidine to create conformationally restricted analogs
Outcome: 3x increase in plasma half-life vs. first-generation compounds

Case 2: PROTAC Degrader Optimization

Challenge: Reduce off-target effects in BTK degraders
Solution: Incorporated chiral piperidine core for precise E3 ligase engagement
Outcome: Achieved IC₅₀ of 12 nM with >100x selectivity over non-target kinases

4. Technical Synthesis Example

Cyclization Protocol for Amino-Oxazolidinones

1. Dissolve 5.0 g (R)-1-Boc-3-Hydroxypiperidine in anhydrous DCM (50 mL)
2. Add 1.2 eq. imidazole under N₂ at 0°C
3. Slowly introduce 1.5 eq. SOCl₂ via syringe pump (30 min addition)
4. Warm to RT and stir for 4 hr (TLC monitoring)
5. Quench with sat. NaHCO₃, extract 3x with EA
6. Dry (Na₂SO₄) and concentrate to yield 4.3 g (82%) cyclized product

5. Client Success Stories

Top-tier Biopharma Company

“Used (R)-1-Boc-3-Hydroxypiperidine in our KRAS inhibitor program. The material’s consistent quality enabled rapid SAR development, leading to clinical candidate selection in 11 months.”

Academic Research Group

“Critical for our work on allosteric GPCR modulators. The chiral purity allowed isolation of single diastereomers in multi-step sequences.”

6. Contact for Custom Solutions

For bulk quantities, custom derivatives, or technical support:
Email: info@vivalr.com
Tel: (86) 15866781826
Provide your project requirements for tailored synthesis protocols and scale-up support.