C07C2602/24

MULTI- OR DUAL-HEADED COMPOSITIONS USEFUL FOR CHAIN SHUTTLING AND PROCESS TO PREPARE THE SAME
20190225719 · 2019-07-25 ·

The present disclosure relates to a multi- or dual-headed composition having the formula (I) or (II). The present disclosure also relates to a process for preparing the multi- or dual-headed composition having the formula (I) or (II), the process including combining 1,2,4-trivinylcyclochexane, an organometallic compound, and a catalyst precursor. The present disclosure further relates to use of the composition having the formula (I) or (II) in olefin polymerization.

Methods of manufacturing treprostinil and treprostinil derivative prodrugs

Methods for making prodrugs of trepreostinil and treprostinil derivatives are provided. Specifically, methods are provided herein for producing prostacyclin compounds comprising treprostinil covalently linked to a linear C.sub.5-C.sub.18 alkyl, branched C.sub.5-C.sub.18 alkyl, linear C.sub.2-C.sub.18 alkenyl, branched C.sub.3-C.sub.18 alkenyl, aryl, aryl-C.sub.1-C.sub.18 alkyl or an amino acid or a peptide (e.g., dipeptide, tripeptide, tetrapeptide). The linkage, in one embodiment, is via an amide or ester bond. Prostacyclin compounds provided herein can also include at least one hydrogen atom substituted with at least one deuterium atom. The compounds provided herein can be used to treat pulmonary hypertension (e.g., pulmonary arterial hypertension) and portopulmonary hypertension.

Methods for improved production of vitamins D2 and D3
10336694 · 2019-07-02 · ·

It is an object of the present invention to provide methods for producing vitamin D that gives improved yields and reduced side product contamination. In various aspects, these methods provide for production of vitamin-D.sub.2 using ergosterol as provitamin D.sub.2 or a dihydroxy derivative thereof as a starting material, or production of vitamin-D.sub.3 using 7-dehydrocholesterol as provitamin D.sub.3 or a dihydroxy derivative thereof as the starting material. The methods described herein comprise irradiating the starting material in a solution including an organic or inorganic base with light in the wavelength range 245-360 nanometers (nm) to obtain a product containing pre-vitamin-D.sub.2 or pre-vitamin-D.sub.3, and heating the product to convert the resulting pre-vitamin-D.sub.2 or pre-vitamin-D.sub.3 to vitamin D.sub.2 or vitamin D.sub.3. In various embodiments, these methods further comprise recovering vitamin D.sub.2 or vitamin D.sub.3 from this reaction as a purified product.

Process For Preparing Pleuromutilin
20190106400 · 2019-04-11 ·

The present disclosure provides processes for preparing (+)-pleuromutilin and synthetic (+)-pleuromutilin produced therefrom. Also provided are intermediates prepared thereby and processes for preparing these intermediates.

Process for producing 7-dehydrocholesterol and vitamin D3

According to the present invention, there can be provided A process for producing 7-dehydrocholesterol (hereinafter, 7DHC), comprising culturing, in a medium, a 7DHC-producing Labyrinthulea microorganism in which the 7DHC reducing activity is reduced or lost as compared to a parent strain through deletion, substitution, or addition of at least one base in a gene which is present in the chromosomal DNA of the parent strain and encodes a protein having 7DHC reducing activity, and the microorganism produces 7DHC, allowing 7DHC to be produced and accumulated in the culture, and collecting the 7DHC from the culture; and a process for producing vitamin D3, comprising irradiating, with ultraviolet light, the 7DHC produced by the production process.

25-OH VITAMIN D DERIVATIVES FOR DETERMINING VITAMIN D METABOLITES
20190101548 · 2019-04-04 · ·

The present invention relates to new vitamin D compounds which are bonded to a labelling group at the C3 stereocentre by means of a linker. The present invention further relates to a method for producing these vitamin D compounds and to the use of an intermediate for producing these compounds. The present invention also relates to a method for quantitatively determining vitamin D using a vitamin D compound according to the invention as a tracer. Furthermore, the present invention relates to a reagent for determining vitamin D, containing a compound according to the invention, and to the use thereof for determining vitamin D.

Fused cyclooctyne compounds and their use in metal-free click reactions

The invention relates to fused cyclooctyne compounds, and to a method for their preparation. The invention also relates to a conjugate wherein a fused cyclooctyne compound according to the invention is conjugated to a label, and to the use of these conjugates in bioorthogonal labeling, imaging and/or modification, such as for example surface modification, of a target molecule. The invention further relates to a method for the modification of a target molecule, wherein a conjugate according to the invention is reacted with a compound comprising a 1,3-dipole or a 1,3-(hetero)diene.

Acetylenic cyanoenones as therapeutics for inflammation and carcinogenesis

The present invention provides a compound having the structure: ##STR00001##
wherein X is C.sub.1-C.sub.12 alkyl, C.sub.2-C.sub.12 alkenyl, C.sub.2-C.sub.12 alkynyl, cyano, aryl, heteroaryl, alkylaryl, alkylheteroaryl, alkenylaryl, alkenylheteroaryl, alkynylaryl, alkynylheteroaryl, alkoxy, alkenyloxy, alkynyloxy, aryloxy, heteroaryloxy, acyl, alkylhydroxy, alkylamino, alkenylamino, alkynylamino, amido, carboxyl, or carboxyl ester, or forms an unsubstituted or substituted cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, indane or tetralin with Y, Y is H or forms an unsubstituted or substituted cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, indane or tetralin with X, or forms an unsubstituted or substituted monocycle with Z; and Z is H or forms an unsubstituted or substituted monocycle with Y; wherein when X and Y are both H, then X is C.sub.2 alkenyl or C.sub.2 alkynyl, and when Y is H forms a substituted cyclohexyl, cycloheptyl with X, the cyclohexyl is other than a trisubstituted cyclohexyl bearing CH.sub.3, i-Pr and (CH.sub.2).sub.2CO.sub.2CH.sub.3 groups or CH.sub.3, i-Pr and (CH.sub.2).sub.3NH.sub.2,
or a salt or ester thereof.

TETRACYCLINE COMPOUNDS

The present invention is directed to a compound represented by Structural Formula (I):

##STR00001##

or a pharmaceutically acceptable salt thereof. The variables for Structural Formula I are defined herein.

Also described is a pharmaceutical composition comprising the compound of Structural Formula I and its therapeutic use.

25-OH vitamin D derivatives for determining vitamin D metabolites
10222388 · 2019-03-05 · ·

The present invention relates to new vitamin D compounds which are bonded to a labelling group at the C3 stereocentre by means of a linker. The present invention further relates to a method for producing these vitamin D compounds and to the use of an intermediate for producing these compounds. The present invention also relates to a method for quantitatively determining vitamin D using a vitamin D compound according to the invention as a tracer. Furthermore, the present invention relates to a reagent for determining vitamin D, containing a compound according to the invention, and to the use thereof for determining vitamin D.