Dow Agrosciences LLC

Eli Lilly and Company

Other

Peter S Borromeo

Carl Vincent DeAmicis

Daniel Knueppel

Gregory T Whiteker

Ricky Hunter

Tony K Trullinger

Ronald Ross, Jr

Gary A Roth

Yu Zhang

Noormohamed Mohamed Niyaz

David Anthony Demeter

Ann Marie Buysse

Christian Thomas Lowe

Akshay Patny

Nakyen Choy

Negar Garizi

Paul Renee LePlae, Jr

Asako Kubota

Martin J Walsh

Frank J Wessels

Nicholas R Babij

Stephen A Hitchcock

Timothy Alan Shepherd

Louis Nickolaus Jungheim

Matthias Stefan Ober

William W Turner

William Wilson Turner, Jr

Jeffrey Daniel Cohen

Daniel Ray Mayhugh

Patrick S Hanley

George Stuart Gregory

Stacy Kay Henle

Tina Staton

Nicole Hough

Grant Von Wald

Gary D Crouse

Michael J Rodriguez

Fangzheng Li

Lawrence C Creemer

James Andrew Jamison

Venkatraghaven Vasudevan

A fungicidal 4-methoxy-3-acetyloxypicolinamide may be conveniently prepared in processes that include the coupling together of 4-methoxy-3-acetyloxypicolinic acid or 4-methoxy-3-hydroxypicolinic acid with a key 2-aminopropanoate ester derived from a 1,1-bis(4-fluorophenyl)propane-1,2-diol.

Processes for the preparation of 4-alkoxy-3-(acyl or alkyl)oxypicolinamdes

4-Alkoxy-3-hydroxypicolinic acids may be conveniently prepared from 4,6-dibromo-3-hydroxypicolinonitrile in a series of chemical steps selected from bromo substitution, nitrile hydrolysis and halogen reduction that are conducted as a single pot process. 4,6-Dibromo-3-hydroxypicolinonitrile may be prepared from furfural in a series of chemical steps selected from cyano-amination, amine salt formation and bromination-rearrangement. 4-Alkoxy-3-acetoxypicolinic acids may be conveniently prepared from 4-alkoxy-3-hydroxypicolinic acids by treatment with acetic anhydride.

Process for the preparation of 4-alkoxy-3-acetoxypicolinic acids

Processes for the preparation of 4-alkoxy-3-(acyl or alkyl)oxypicolinamides

By either forming a triaryl acid halide or a triaryl mixed anhydride and subsequently treating with aqueous sodium azide, triaryl acyl azides are prepared in high yield using inexpensive reagents in a process in which by-products are easily removed from the triaryl acyl azide.

Process for preparation of 4-(1-(4-(perfluoroethoxy)phenyl)-1H-1,2,4-triazol-3-yl)benzoyl azide

This document discloses molecules having the following formula ('Formula One'): and processes related thereto.

Pesticidal compositions and processes related thereto

Triaryl rhamnose carbamate insecticides are prepared from triaryl acyl azides and tetrahydropyran-2-ols in good yield without the use of a hydride base.

Process for the preparation of certain triaryl rhamnose carbamates

A method for modifying the cyclic peptide ring system of Echinocandin-type compounds to produce new analogs having antifungal activity is provided. The inventive process comprises opening the cyclic peptide ring, cleaving the terminal ornithine unit, inserting at least one new amino acid or other synthetic unit and closing the ring to produce a new cyclic peptide ring structure. The process allows one to incorporate features such as water-solubility into the cyclic peptide ring nucleus, sites for further modification, increase or decrease the number of amino acid or peptide units within the ring nucleus, and increase or decrease the total number of members within the ring. The invention further provides novel Echinocandin type compounds and their use as antifungal or anti-parasitic agents.

Ring modified cyclic peptide analogs

A method for modifying the cyclic peptide ring system of Echinocandin-type compounds to produce new analogs having antifungal activity is provided. The inventive process comprises opening the cyclic peptide ring, cleaving the terminal omithine unit, inserting at least one new amino acid or other synthetic unit and closing the ring to produce a new cyclic peptide ring structure. The process allows one to incorporate features such as water-solubility into the cyclic peptide ring nucleus, sites for further modification, increase or decrease the number of amino acid or peptide units within the ring nucleus, and increase or decrease the total number of members within the ring. The invention further provides novel Echinocandin type compounds and their use as antifungal or anti-parasitic agents.

Provided are pharmaceutical formulations, and methods of inhibiting fungal and parasitic activity using a compound of formula I ##STR1## where: R', R', R'', R.sup.x1, R.sup.x2, R.sup.y1, R.sup.y2, R.sup.y3, R.sup.y4, and R.sup.0 are as defined above; and

Cyclic peptide antifungal agents and methods of making and using

Provided are pharmaceutical formulations, and methods of inhibiting fungal and parasitic activity using a compound of formula I: ##STR1## wherein: R' is hydrogen, methyl or NH.sub.2 C(O)CH.sub.2 --;

Cyclic peptide antifungal Agents

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Fishers, IN, United States of America

Peter S Borromeo