C07D493/22

Pyran fused ring compound, preparation method therefor and use thereof

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.

NOVEL COMPOUND AND ORGANIC LIGHT EMITTING DEVICE COMPRISING THE SAME

Provided is compound of Chemical Formula 1:

##STR00001## wherein: each X.sub.1 is independently N or CH, provided that at least one of them is N; each X.sub.2 is independently N or CH, provided that at least one of them is N; Ar.sub.1 to Ar.sub.4 are each independently a substituted or unsubstituted C.sub.6-60 aryl or a substituted or unsubstituted C.sub.5-60 heteroaryl containing one or more of N, O, and S; Ar.sub.5 is a substituted or unsubstituted C.sub.6-60 aryl or a substituted or unsubstituted C.sub.5-60 heteroaryl containing one or more of N, O, and S; each R.sub.1 is independently hydrogen, deuterium, a substituted or unsubstituted C.sub.1-60 alkyl, a substituted or unsubstituted C.sub.3-60 cycloalkyl, a substituted or unsubstituted C.sub.6-60 aryl, or a substituted or unsubstituted C.sub.5-60 heteroaryl containing one or more of N, O, and S; and n is an integer of 0 to 4,
and an organic light emitting device including the same.

CHLOROTONIL DERIVATIVES

The present invention relates to novel chlorotonil derivatives of formula (I) and the use thereof for the treatment or prophylaxis of bacterial infections and malaria.

##STR00001##

GINKGOLIDE B DERIVATIVE AND SALT THEREOF, PREPARATION METHOD THEREFOR AND USE THEREOF

The present invention relates to the technical field of medicine, and to derivatives represented by formula 1 and formula 2 in which a carboxylic acid group is introduced into the structure of Ginkgolide B by means of a hydroxyl group at the 10-position and ester derivatives of carboxylic acid groups, and pharmaceutically acceptable organic or inorganic salts. Ginkgolide B is used as a parent body and is prepared by means of chemical structure modification so as to achieve the goals of improving solubility, increasing bioavailability and enhancing healing efficacy. The prepared compound and carboxylate salts thereof have significant platelet activating factor antagonism, an anticoagulant effect and an anti-acute cerebral ischemia effect, and can be used for preparing a drug for preventing and treating ischemic stroke, thrombosis, angina pectoris, cardiopulmonary infarction, as well as inflammation, asthma and other diseases related to a platelet activating factor.

##STR00001##

GINKGOLIDE B DERIVATIVE AND SALT THEREOF, PREPARATION METHOD THEREFOR AND USE THEREOF

The present invention relates to the technical field of medicine, and to derivatives represented by formula 1 and formula 2 in which a carboxylic acid group is introduced into the structure of Ginkgolide B by means of a hydroxyl group at the 10-position and ester derivatives of carboxylic acid groups, and pharmaceutically acceptable organic or inorganic salts. Ginkgolide B is used as a parent body and is prepared by means of chemical structure modification so as to achieve the goals of improving solubility, increasing bioavailability and enhancing healing efficacy. The prepared compound and carboxylate salts thereof have significant platelet activating factor antagonism, an anticoagulant effect and an anti-acute cerebral ischemia effect, and can be used for preparing a drug for preventing and treating ischemic stroke, thrombosis, angina pectoris, cardiopulmonary infarction, as well as inflammation, asthma and other diseases related to a platelet activating factor.

##STR00001##

INTERMEDIATE OF ERIBULIN AND SYNTHESIS METHOD AND USE THEREOF
20220204523 · 2022-06-30 ·

An intermediate compound is prepared and used for the synthesis of halichondrin B, eribulin or an analog thereof, particularly a structural fragment C27-C35 thereof. The starting materials of the synthetic route are readily available, and the optical purity of the starting materials can be ensured, so that the optical purity of the structural fragment C27-C35 in halichondrin B, eribulin or the analog thereof is ensured. Steps for constructing a chiral center of the structural fragment C27-C35 feature higher diastereoselectivity and yield, in particular preparation methods of compounds of formulae (X), (XI), (XVI) and (XV). By-products of partial reactions can be removed only by recrystallization, which results in easy purification and significant reduce in cost.

INTERMEDIATE OF ERIBULIN AND SYNTHESIS METHOD AND USE THEREOF
20220204523 · 2022-06-30 ·

An intermediate compound is prepared and used for the synthesis of halichondrin B, eribulin or an analog thereof, particularly a structural fragment C27-C35 thereof. The starting materials of the synthetic route are readily available, and the optical purity of the starting materials can be ensured, so that the optical purity of the structural fragment C27-C35 in halichondrin B, eribulin or the analog thereof is ensured. Steps for constructing a chiral center of the structural fragment C27-C35 feature higher diastereoselectivity and yield, in particular preparation methods of compounds of formulae (X), (XI), (XVI) and (XV). By-products of partial reactions can be removed only by recrystallization, which results in easy purification and significant reduce in cost.

Chlorotonil derivatives

The present invention relates to novel chlorotonil derivatives of formula (I) and the use thereof for the treatment or prophylaxis of bacterial infections and malaria. ##STR00001##

Novel Compounds and Pharmaceutical Preparations

Extracts and pharmaceuticals form Neobeguea mahafalensis, the procedures for their preparation, and their use for eliciting sexual enhancing effect and for treatment of sexual dysfunction, in particular erectile dysfunction and hypoactive desire disorders are disclosed. The structures of the chemical compounds in these extracts causing sexual enhancing effect, the preparation of these compounds and the pharmaceuticals prepared from them are disclosed.

Novel Compounds and Pharmaceutical Preparations

Extracts and pharmaceuticals form Neobeguea mahafalensis, the procedures for their preparation, and their use for eliciting sexual enhancing effect and for treatment of sexual dysfunction, in particular erectile dysfunction and hypoactive desire disorders are disclosed. The structures of the chemical compounds in these extracts causing sexual enhancing effect, the preparation of these compounds and the pharmaceuticals prepared from them are disclosed.