Alphora Research Inc.

Sandoz Ag

Ming Pan

Fabio E S Souza

Boris Gorin

Alena Rudolph

Ricardo Orprecio

Huzaifa Rangwala

Fabio Es Souza

Dino Alberico

Jason A Bexrud

Fabio Eduardo Silva E Souza

Kathleen Da Silva Turcot

Teng Ko Ngooi

Jason Edward Field

Robert Jordan

Navindra Jainarine Ramjit

Tharsika Tharmanathan

Tracey Jende-Tindall

Fabio ES Souza

Disclosed are salts of 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 the salts of the compounds of formula 1, and intermediates used therein. The salts of the compound of formula 1 can be useful for preparation of halichondrin analogs such as eribulin. 

Crystalline derivatives of (S)-1-((2R,3R,4S,5S)-5-allyl-3-methoxy-4-(tosylmethyl)tetrahydrofuran-2-YL)-3-aminopropan-2-ol

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. 

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Synthetic process for preparation of macrocyclic C1-keto analogs of halichondrin B and intermediates useful therein

The specification relates to compounds and process for the preparation of a compound of formula 7, where LG is a leaving group and hal is a halide and is Cl, Br or I. The compound of formula 7 can be useful in the preparation of natural products, such as halichondrin and its derivatives.

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

Paricalcitol, a synthetic vitamin D analog, is purified to a purity greater than 99.7% by crystallization from solution in isopropyl acetate solvent, followed by filtration and vacuum drying. Isopropyl acetate appears to be unique among commonly available and pharmaceutically acceptable solvents in its ability to precipitate paricalcitol in this high purity, essentially free of isomers thereof. In addition, paricalcitol of purity of at least 99.9% has been shown to have exceptional storage stability.

Paricalcitol purification

Paricalcitol, a synthetic vitamin D analog, is purified to a purity greater than 99.7% by crystallization from solution in isopropyl acetate solvent, followed by filtration and vacuum drying. Isopropyl acetate appears to be unique among commonly available and pharmaceutically acceptable solvents in its ability to precipitate paricalcitol in this high purity, essentially free of isomers thereof.

Dronabinol, the tetrahydrocannabinol compound which comprises the active constituent of marijuana and is pharmaceutically useful as an antiemetic, is prepared by a process involving reaction of cis-menth-1-enc-3,8-diol with olivetol to form 1,3-dihydroxy-2-[(1R,6R)-6-(2-hydroxyprop-2-yl)-3-methylcyclohex-2-en-1-yl]-5-pentylbenzene; and cyclizing the 1,3-dihydroxy-2-[(1R,6R)-6-(2-hydroxyprop-2-yl)-3-methylcyclohex-2-en-1-yl]-5-pentylbenzene so formed to obtain dronabinol. A novel synthesis of cis-menth-1-ene-3,8-diol is also provided.

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Mississauga, Canada

Ming Pan