C07D493/22

PYRAN FUSED RING COMPOUND, PREPARATION METHOD THEREFOR AND USE THEREOF
20220048921 · 2022-02-17 ·

The present invention relates to pyran-fused ring compounds, preparation methods thereof and use thereof, especially to pyran-fused ring compounds usable for preparing Halichondrin, Eribulin, or analogues thereof, preparation methods thereof and use thereof. Use of any of the compounds of formula (I) to (XIII) of the present invention in preparation of Halichondrin B, Eribulin, analogues thereof or C1-C13 moieties thereof. Provided in the present invention are intermediates usable for preparing Halichondrin B, Eribulin, or analogues thereof, especially the key product of C1-C13 moieties, preparation methods thereof and use thereof. The starting material for the synthesis pathway of the present invention is inexpensive and readily available with sustainable source and reliable quality. Since the structural characteristics of the reactants of theirself are made full use in choosing the method of constructing the chiral centers, the efficiency in the synthesis is considerably increased, the difficulty in and the risk on quality control of the product are reduced; and using a highly toxic and expensive high-valent osmium catalyst is avoided, which have the cost and environmental friendliness significantly improved.

SHORT SYNTHESES OF (-)-PICROTOXININ AND RELATED COMPOUNDS

The present disclosure relates to concise processes for making (−)-picrotoxinin (1, PXN) and 5-methyl-picrotoxinin (20, 5MePXN), and to 5MePXN, its pharmaceutical compositions, and its method of use for inhibiting GABA.sub.A receptor.

PROCESS FOR THE PREPARATION OF MACROCYCLIC KETONE ANALOGS OF HALICHONDRIN B OR PHARMACEUTICALLY ACCEPTABLE SALTS AND INTERMEDIATES THEREOF

The present invention discloses a novel process for the preparation of macrocyclic ketone analogs of halichondrin B or pharmaceutically acceptable salts thereof and to novel intermediates which are produced during the course of carrying out the novel process.

PROCESS FOR THE PREPARATION OF MACROCYCLIC KETONE ANALOGS OF HALICHONDRIN B OR PHARMACEUTICALLY ACCEPTABLE SALTS AND INTERMEDIATES THEREOF

The present invention discloses a novel process for the preparation of macrocyclic ketone analogs of halichondrin B or pharmaceutically acceptable salts thereof and to novel intermediates which are produced during the course of carrying out the novel process.

STEREOCHEMICALLY DEFINED POLYPROPIONATES AND METHODS FOR MAKING AND USING THE SAME

The present invention relates to stereochemically defined polypropionates and methods for preparing and using the same. The stereochemically defined polypropionates may be useful in the synthesis of natural products and/or natural product-like libraries.

STEREOCHEMICALLY DEFINED POLYPROPIONATES AND METHODS FOR MAKING AND USING THE SAME

The present invention relates to stereochemically defined polypropionates and methods for preparing and using the same. The stereochemically defined polypropionates may be useful in the synthesis of natural products and/or natural product-like libraries.

BRYOSTATIN ANALOGS AND USE THEREOF AS ANTIVIRAL AGENTS

Described herein are tricyclic macrolactones. The macrolactones have a high binding affinity for PKC. The compounds described herein can be used in a number of therapeutic applications including the treatment or prevention of viral infection. Also described herein are methods for producing macrolactones. The methods permit the high-yield synthesis of macrolactones in a low number of steps and with a high degree of substitution and specificity.

SYNTHESIS OF NANOTUBULAR MOLECULES

A method of creating a tubular compound includes providing an end cap including a macrocycle that is sufficiently rigid that it presents a plurality of functional groups oriented axially on or extending axially from a first axial side of the end cap, creating a tubular wall from a plurality of reactive compounds which is covalently attached to the end cap via reaction of the plurality of functional groups extending from the first axial side of the end cap, the tubular wall extending axially from the first axial side end cap, and performing at least one equatorial cyclization reaction axially distant from the end cap which includes covalent bonding of residues of a group of the plurality of reactive compounds used in forming the tubular wall.

SYNTHESIS OF NANOTUBULAR MOLECULES

A method of creating a tubular compound includes providing an end cap including a macrocycle that is sufficiently rigid that it presents a plurality of functional groups oriented axially on or extending axially from a first axial side of the end cap, creating a tubular wall from a plurality of reactive compounds which is covalently attached to the end cap via reaction of the plurality of functional groups extending from the first axial side of the end cap, the tubular wall extending axially from the first axial side end cap, and performing at least one equatorial cyclization reaction axially distant from the end cap which includes covalent bonding of residues of a group of the plurality of reactive compounds used in forming the tubular wall.

Bisbenzofuran-fused indeno[1,2-B]fluorene derivatives and related compounds as materials for organic electroluminescent devices (OLED)

The present invention relates to Bisbenzofuran-fused indeno[1,2-b]fluorene derivatives and related compounds as materials for organic electroluminescent devices (OLEDs).