Millennium Pharmaceuticals Limited

Biocon Limited

Anegondi Sreenivasa Prasad

Mukund Shankar Chorghade

Vemuri Venkata Kiran Rao

Amin Ul Islam

Mukund Keshao Gurjar

Sunil Vyankatesh Mhaskar

Kiran Kumar Kothakonda

Alla Venkata Rama Rao

Batchu Venkateswara Rao

Srinivas Pullela Venkata

Ganesh Ekambaram

Alla Verkata Rama Rao

Lalata Krishnakanth Reddy

Ranga Reddy

Kotakonda Shailaja

Srinivas Pullela, Venkata

The present disclosure discloses processes of Everolimus and intermediates: reacting Sirolimus (Rapamycin) under solvent free conditions with appropriate side chain implying portion wise additions, one pot conversion, and resin mediated synthesis.

Processes for preparation of Everolimus and intermediates thereof

A method is provided for synthesizing diaryl-substituted heterocyclic compounds, particularly 2,5-diaryl-substituted tetrahydrofurans and tetrahydrothiophenes. Methods for synthesizing starting materials and intermediates are provided as well. An important application of the invention is in the synthesis of CMI-392, (&plusmn;)trans-2-&lsqb;5-N&prime;-methyl-N&prime;-hydroxyureidyl-methyl)3-methoxy-4-p-chlorophenylthioethoxyphenyl&rsqb;-5-(3,4,5-trimethoxyphenyl)-tetrahydrofuran, a highly effective agent in treating inflammatory and immune disorders. The invention also encompasses novel compounds useful as starting materials and intermediates in the synthetic processes disclosed.

Method for synthesizing diaryl-substituted heterocyclic compounds, including tetrahydrofurans

A method is provided for synthesizing diaryl-substituted heterocyclic compounds, particularly 2,5-diaryl-substituted tetrahydrofurans and tetrahydrothiophenes. Methods for synthesizing starting materials and intermediates are provided as well. An important application of the invention is in the synthesis of CMI-392, (&plusmn;) trans-2-&lsqb;5-(N&prime;-methyl-N&prime;-hydroxyureidyl-methyl)-3-methoxy-4-p-chlorophenylthioethoxyphenyl&rsqb;-5-(3,4,5-thrimethoxyphenyl)-tetrahydrofuran, a highly effective agent in treating inflammatory and immune disorders. The invention also encompasses novel compounds useful as starting materials and intermediates in the synthetic processes disclosed.

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Hyderabad Telangana, India

Anegondi Sreenivasa Prasad