Synthesis of Thiazines, Thiazinones and N-Cycloalkyl Azoles Via Novel Synthetic Routes

Title

Synthesis of Thiazines, Thiazinones and N-Cycloalkyl Azoles Via Novel Synthetic Routes

Creator

Polina, Sai Babu

Contributor

Prasad, Pralhad Pujar

Description

Heterocyclic building blocks have gained the utmost importance in recent past on the newlineaccount of their significance in biological and pharmaceutical fields. Among these newlinenitrogen and sulphur containing heterocyclic building blocks such as thiazines, newlinethiazinones and N-cycloalkyl heterocyclic motifs hold an important role in medicinal newlinechemistry. Thiazine cores are used for the treatment of various life threating diseases newlinelike cancer, cardiovascular and fabry diseases. Drugs containing thiazinone cores were used to treat Parkinson, Alzheimer s and various neuro degenerative diseases. Ncycloalkyl azole motifs are used to treat various life threating cancers like neck, lung, prostate, breast etc. As per the literature review, synthesis of these motifs are done using multi steps and harsh conditions, which limited the substrate scope. In this thesis we describe our studies on development of one pot, mild condition for newlinesynthesis of thiazinone cores using P(NMe2)3 (HMPT). We had developed HMPT [P(NMe2)3] mediated reactions towards synthesis of Carbon-Nitrogen/Carbon-Sulphur bond. The developed methodology was extended for thiazine cores as well. This new synthetic methodology is useful to synthesize various N, S-heterocycles including the novel spiro molecules. HMPT reagent under the mild and aerobic reaction conditions provided the access for many manifold immense molecules. Molecular docking studies were conducted for the synthesized compounds considering MOA-B inhibitors as target. MOA-B inhibitor motifs were approved for the treatment of Parkinson illness. The synthesized thiazine and thiazinone molecules showed good binding affinity in molecular docking studies conducted. We had developed a new strategy using T3P (1-Propanephosphonic anhydride, ~ 50 % wt, in EA solution) mediated synthetic procedure for the synthesis of N-cycloalkyl newlineazoles.

Source

Author's Submission

Date

2023-01-01

Publisher

Christ(Deemed to be University)

Subject

Chemistry

Rights

Open Access

Relation

61000278

Format

PDF

Language

English

Type

PhD

Identifier

http://hdl.handle.net/10603/533970