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Industrial Research And Consultancy Centre
Patent
A Process for Synthesis of Bicyclic Ketals
Abstract

This invention presents a method for synthesizing bicyclic ketals efficiently, addressing the need for diverse flavanoid frameworks. The process involves reacting salicylaldehyde with ketones and trimethyl orthoformate in the presence of acid and solvent, yielding desired products. It offers a simple, scalable solution for producing flavan derivatives with structural precision, catering to pharmaceutical and industrial demands.

Figure (1) formula (I) comprising reacting salicylaldehyde of formula (II) with ketones of formula (III) and trimethyl orthoformate in presence of Lewis/Bronsted acid and organic solvent to form an in-situ intermediate of formula (IV) followed by reaction of (IV) with substituted phenols of formula (V)

Problem Statement

The current methods for synthesizing flavanoid frameworks lack efficiency, speed, and scalability. There is a need for a straightforward process to rapidly produce bicyclic ketals, crucial compounds with diverse applications in pharmaceuticals and industries.

Uniqueness of the Solution
  • One-Pot Synthesis: Unique process synthesizing bicyclic ketals from salicylaldehyde, ketones, and trimethyl orthoformate. Simplifying synthesis, reducing steps and time, crucial for efficient production of flavan derivatives. 
  • Fine-Tuning Cycloaddition: Precise control of dienophile in [4+2] Cycloaddition with o-quinone methides (o-QMs). Enabling selective formation of flavan frameworks with diverse substituents, vital for tailored applications. 
  • Iterative Reaction Cascades: Formation of Diels–Alder adducts generating o-QMs-II, allowing Michael addition reactions. Offers a versatile approach to create diverse singly and doubly linked flavan derivatives, crucial for pharmaceutical and industrial uses.
Prototype Details

The invention currently exists as a scalable chemical synthesis protocol that has been experimentally validated in a laboratory setting.

Current Status of Technology

It is in the basic research or conceptual development stage. While the process has been granted.

Technology readiness level

1

Societal Impact
  • Advances in healthcare through the synthesis of compounds with potential medicinal benefits. 
  • Provides opportunities for the development of eco-friendly and sustainable chemical processes. 
  • Enhances understanding and utilization of natural products for human welfare. 
  • Supports industries aiming to produce high-value compounds efficiently. 
  • Contributes to the economy by fostering innovation and industrial growth.
Applications or Domain

Pharmaceuticals, Healthcare, Chemical industry, Biotechnology, Sustainable chemistry, Industrial production

Geography of IP

Type of IP

Application Number

202121026206

Filing Date
Grant Number

440379

Grant Date
Assignee(s)
Indian Institute of Technology Bombay

IP Themes

**This IP is owned by IIT Bombay**