C07C401/00

COCRYSTALS OF STEROID AND SECOSTEROID COMPOUNDS AND COMPOSITIONS COMPRISING THEM

It is provided a cocrystal of a compound of formula (I) or of a compound formula (II) wherein X and Y are independently selected from —CH.sub.2— and —C(CH.sub.2)—, provided that al least one of X or Y is —CH.sub.2—; R.sup.1 is —CHCH.sub.3—Z.sub.m—W.sub.n—(CH.sub.2).sub.o-T.sub.p-S, wherein Z is O, and m is 0 or 1; W is R.sup.4CH CHR.sup.5, wherein either R.sup.4 and R.sup.5 are H and the dashed line indicates that there is a single bond, or R.sup.4 and R.sup.5 together are forming a bond and the dashed line indicates that there is a double bond, and n is 0 or 1; o is 0, 1 or 3; T is selected from the group consisting of —CHR.sup.6—, —C(O), wherein R.sup.6 is —OH or —CH.sub.3, and p is 0 or 1; S is selected from the group consisting of H, (C.sub.1-C.sub.3) alkyl optionally substituted by —OH, (C.sub.1-C.sub.3) haloalkyl optionally substituted by —OH, cyclopropyl, or; and R.sup.2 is —H or —OH; R.sup.3 is H or CH.sub.3; and the dashed line in formula (II) indicates a single or a double bond; and a hydrogen bond donor coformer which is a phenolic compound. It is also provided a composition comprising the cocrystal and a personal care product comprising the composition.

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Procedure for crystallization of (22E)-(24R)-2-methylene-22-dehydro-1α,24-25-trihydroxy-19-nor-vitamin D.SUB.3

Disclosed are methods of purifying the compound (22E)-(24R)-2-methylene-22-dehydro-1α,24,25-trihydroxy-19-nor-vitamin D.sub.3 to obtain the compound in crystalline form. The methods typically include the steps of dissolving (22E)-(24R)-2-methylene-22-dehydro-1α,24,25-trihydroxy-19-nor-vitamin D.sub.3 in a solvent comprising ethyl acetate and hexane to form a solution, allowing crystals of (22E)-(24R)-2-methylene-22-dehydro-1α,24,25-trihydroxy-19-nor-vitamin D.sub.3 to form and precipitate from the solution, and recovering the crystals of (22E)-(24R)-2-methylene-22-dehydro-1α,24,25-trihydroxy-19-nor-vitamin D.sub.3 from the solution.

Procedure for crystallization of (22E)-(24R)-2-methylene-22-dehydro-1α,24-25-trihydroxy-19-nor-vitamin D.SUB.3

Disclosed are methods of purifying the compound (22E)-(24R)-2-methylene-22-dehydro-1α,24,25-trihydroxy-19-nor-vitamin D.sub.3 to obtain the compound in crystalline form. The methods typically include the steps of dissolving (22E)-(24R)-2-methylene-22-dehydro-1α,24,25-trihydroxy-19-nor-vitamin D.sub.3 in a solvent comprising ethyl acetate and hexane to form a solution, allowing crystals of (22E)-(24R)-2-methylene-22-dehydro-1α,24,25-trihydroxy-19-nor-vitamin D.sub.3 to form and precipitate from the solution, and recovering the crystals of (22E)-(24R)-2-methylene-22-dehydro-1α,24,25-trihydroxy-19-nor-vitamin D.sub.3 from the solution.

GLUCOCORTICOID RECEPTOR MODULATORS
20230212215 · 2023-07-06 ·

The present disclosure relates to polycyclic (e.g., tetracyclic) glucocorticoid receptor (GR) modulators, synthetic methods for preparing such GR modulators, and methods of using such GR modulators to treat a glucocorticoid-dependent condition, such as cancer or hypercortisolism. Exemplary compounds have quaternary centers at C9 and C13 in which the quaternary center at C9 projects a substituent on the opposite face of the tetracycle as the substituent at C13.

Methods for assembly of tetracyclic compounds by stereoselective C9-C10 bond formation
11512107 · 2022-11-29 · ·

The present disclosure relates to stereodefined polycyclic (e.g., tetracyclic) compounds that contain quaternary centers at one or multiple ring fusions, synthetic methods for preparing such compounds, and methods of using such compounds to treat a disease, such as a brain tumor and, particularly, a glioma.

SYNTHESIS OF CHOLESTEROL AND VITAMIN D3 FROM PHYTOSTEROLS

The present invention discloses novel method for synthesizing vegan cholesterol and vitamin D3 from inexpensive crude phytosterol.

SYNTHESIS OF CHOLESTEROL AND VITAMIN D3 FROM PHYTOSTEROLS

The present invention discloses novel method for synthesizing vegan cholesterol and vitamin D3 from inexpensive crude phytosterol.

Process and intermediates for the preparation of eldecalcitol

The invention relates to new intermediates in the synthesis of Eldecalcitol and to processes for the preparation of said intermediates and of Eldecalcitol.

Process and intermediates for the preparation of eldecalcitol

The invention relates to new intermediates in the synthesis of Eldecalcitol and to processes for the preparation of said intermediates and of Eldecalcitol.

25-hydroxycholecalciferol monohydrate crystal, preparation method therefor and microemulsion using same

A 25-hydroxycholecalciferol monohydrate crystal, a preparation method thereof, and a microemulsion using the 25-hydroxycholecalciferol monohydrate crystal. The X-ray powder diffraction spectrum of the 25-hydroxycholecalciferol monohydrate crystal of the present disclosure shows characteristic peaks at 2θ of 10.035°, 11.623°, 14.631°, 15.054°, 15.551°, 16.471°, 17.198°, 19.002°, 19.628°, 20.109°, 21.886°, 23.113°, 23.661°, 24.701°, 25.220°, 25.440°, and 28.527°. The 25-hydroxycholecalciferol monohydrate crystal can effectively enhance the stability of 25-hydroxycholecalciferol, and is more beneficial to the production and storage of related preparations, and thus biological characteristics of 25-hydroxycholecalciferol can be effectively utilized.