Alphora Research Inc.

Sandoz Ag

Aerpio Therapeutics, Inc.

Dino Alberico

Boris Gorin

Joshua Clayton

Jan Oudenes

Craig Edward Dixon

Fabio E S Souza

Ming Pan

Alena Rudolph

Robert Jordan

Fabio Es Souza

Ryan Beharrilall

Varghese Rexon

Gorin Boris

Joshua A Clayton

Fabio ES Souza

Disclosed is a compound of formula 1, or a pharmaceutically acceptable salt thereof, where R, R, R, R, R, R, R, R, R, R, R, R, Rand Rare as disclosed herein. Also, disclosed is a process for the preparation of the compound of formula 1, or a pharmaceutically acceptable salt thereof, and intermediates used therein. The compound of formula 1 can be used in the preparation of halichondrin analogs, such as Eribulin; and a process for its preparation from the compound of formula 1 is also disclosed. 

[object Object]

Disclosed is a process for preparing a carbonucleoside of formula (1) and intermediates for use therein. The process involves the step of reacting a compound of formula (2) with a compound of formula (3) under Mitsunobu-type reaction conditions to obtain a compound of formula (4), wherein PG, PG, PGand PGare protecting groups. The compound of formula (4) is deprotected to form the compound of formula (1), as shown below. 

Process for the synthesis of carbonucleoside and intermediates for use therein

Disclosed herein is a process for preparing N-benzyl-3-hydroxypyridin-2-(1H)-ones that are substituted at the pyridine ring 4-position with a 4-carbamoylpiperazin-1-yl moiety.

Process for preparing N-benzyl-3-hydroxy-4-substituted-pyridin-2-(1H)-ones

Disclosed is a compound of formula 1, as shown below, where R, R, R, R, R, Rand Rare as described herein. Also, disclosed is a process for the preparation of compounds of formula 1, and intermediates used therein. The compound of formula 1 can be useful for preparation of halichondrin analogs such as Eribulin. 

2-((2S,3S,4R,5R)-5-((S)-3-amino-2-hydroxyprop-1-yl)-4-methoxy-3-(phenylsulfonylmethyl)tetrahydrofuran-2-yl)acetaldehyde derivatives and process for their preparation

Anti-virally active carbanucleosides such as entecavir are prepared by a process which utilizes, throughout the synthesis, an aromatic protectant group for the hydroxyl and the alkyl hydroxy groups of the starting material, removed as the final step of a multi-step synthesis. Such protectant groups yield intermediates which are solid and therefore easily purified at various stages of the process, for an economical and relatively fast process for synthesizing the final product.

Carbanucleoside synthesis and novel intermediate compounds useful therein

Fused cyclopentane-4-substituted 3,5-dioxalane lactone compounds useful as an intermediate in the synthesis of prostaglandin analogs are provided. The compounds have the formula A: wherein R represents an aryl group such as p-methoxyphenyl. This compound can be reacted with a lower alkyl aluminum compound to open the dioxalane ring and reduce the lactone to lactol, without over-reducing to diol. The resulting compound can be functionalized to insert chemical side groups of target prostaglandins, adding the required &#x3b1;-side chain and then the required &#x3c9;-side chain sequentially and independently of each other. The compounds and process are particularly suitable for preparing lubiprostone.

Prostaglandin synthesis and intermediates for use therein

Fused cyclopentane&#x2014;4-substituted 3,5-dioxalane lactone compounds useful as an intermediate in the synthesis of prostaglandin analogs are provided. The compounds have the formula A: wherein R represents an aryl group such as p-methoxyphenyl. This compound can be reacted with a lower alkyl aluminum compound to open the dioxalane ring and reduce the lactone to lactol, without over-reducing to diol. The resulting compound can be functionalized to insert chemical side groups of target prostaglandins, adding the required &#x3b1;-side chain and then the required &#x3c9;-side chain sequentially and independently of each other. The compounds and process are particularly suitable for preparing lubiprostone.

Growing community of inventors

Mississauga, Canada

Dino Alberico