Bristol-myers Squibb Compnay

Johnson Matthey Public Limited Company

Karo Bio Ab

Joydeep Kant

Vittorio Farina

Dolatrai M Vyas

Shu-Hui Chen

Jurong Yu

Ramakrishnan Chidambaram

Raymond E Weaver

Arun Ghosh

John F Kadow

Jun Li

David R Langley

Qiufen May Xue

Mark D Wittman

Harold A Mastalerz

Chester Sapino, Jr

Xinhua Qian

Shaopeng Wang

Susan D Boettger

Denis Favreau

Paul R Brodfuehrer

Kathia Levesque

James G Tarrant

Rajendra P Deshpande

Chester Sapino

Jing Liang

Edward J Gublo

Ulhas P Dhokte

Bogdan Mudryk

Brian Leslie James

Frank S Gibson

Karen L TenHuisen

Zhengrong Guo

Thomas R Sattelberg

Vittorio Farino

Provided are processes for the synthesis of aniline derivatives, specifically certain aniline derivatives which have activity as thyroid receptor ligands.

Process for the preparation of aniline-derived thyroid receptor ligands

A process is provided for preparing 4-alkyl- or 4-aryl-oxycarbonyl paclitaxel analogs which includes the steps of converting paclitaxel into a C-7 acylprotected paclitaxel employing an electrophilic protecting group, such as benzoyloxycarbonyl, and converting the C-7 protected analog into the 4-alkyloxycarbonyl or 4-aryloxycarbonyl paclitaxel analog. Novel intermediates produced in the process are also provided.

Process for preparing 4-alkyl- or 4-aryl-oxycarbonyl paclitaxel analogs and novel intermediates

An improved method of synthesis of 21-amino epothilone derivatives which provides a one-pot conversion of 21-hydroxy epothilones to highly desirable 21-amino epothilones in high yield.

Method of preparation of 21-amino epothilone derivatives

A process for the preparation of novel C-4 carbonate taxanes useful as antitumor agents

Process for the preparation of C-4 carbonate taxanes

A process is provided for preparing chiral diol sulfones of the structurewhere Ris preferablywhere Ris preferably aryl such as phenyl, and Ris preferably alkyl such as t-butyl, which are intermediates used in preparing HMG CoA reductase inhibitors.

Process for preparing chiral diol sulfones and dihydroxy acid HMG CoA reductase inhibitors

A process for the synthesis of a C-4 methyl carbonate paclitaxel analog from 10-deacetylbaccatin III by the selective reduction of the acetate at the C-4 position of 10-deacetylbaccatin using Red-Al.

Process for the preparation of a paclitaxel C-4 methyl carbonate analog

A novel process for preparing narcotic analgesics such as hydrocodone and hydromorphone using catalytic amounts of homogeneous organometallic complexes is disclosed.

Preparation of narcotic analgesics

##STR1## in which R.sup.1 is --COR.sup.z in which R.sup.z is RO-- or R;

Deoxy taxols

This invention relates to a fluorinated taxol of formula I ##STR1## in which R.sup.1 is --COR.sup.z in which R.sup.z is RO-- or R;

Fluoro taxols

This invention relates to a novel process for making a cephem of formula II from a 2-(3-amino-2-oxo-azetidin-1-yl)-2,3-butadienoate intermediate of formula I using an organo-copper reagent. In another aspect, this invention is concerned with said intermediate. ##STR1## In the compounds of Scheme (A), R.sup.1 is a conventional amino protecting group or an acyl group; R.sup.2 is an aromatic heterocyclic or aryl group; R.sup.3 is a conventional carboxy protecting group or --CO.sub.2 R.sup.3 taken together forms a physiologically hydrolyzable ester; and R.sup.4 is a group selected from the group consisting of C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, cyclic C.sub.3-6 alkyl, and aryl; and n is 0 or 2.

Processes for making cephems from allenylazetidinone derivatives

This invention relates to a novel process for making a cephem of formula II from a 2-(3-amino-2-oxo-azetidin-1-yl)-2,3-butadienoate intermediate of formula I using an organo-copper reagent. In another aspect, this invention is concerned with said intermediate. ##STR1## In the compounds of Scheme (A), R.sup.1 is a conventional amino protecting group or an acyl group; R.sup.2 is an aromatic heterocyclic or aryl group; R.sup.3 is a conventional carboxy protecting group or --CO.sub.2 R.sup.3 taken together forms a physiologically hydrolyzable ester; and R.sup.4 is a group selected from the group consisting of C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, cyclic C.sub.3-6 alkyl, and aryl; and n is 0 or 2. This invention also relates to an intermediate represented by formula ##STR2## in which R.sup.1, R.sup.2, R.sup.3 and n are as defined above.

Cephalosporin intermediates having a replacable organosulfonylyoxy or heterocyclothio group in the 3-position undergo a carbon alkylation process with organocopper reagents to provide 3-hydrocarbon substituted cephalosporin antibiotics.

Process for production of cephalosporins

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Cherry Hill, NJ, United States of America

Joydeep Kant