57 results about "Eribulin" patented technology

The invention provides an intermediate for preparing eribulin and a preparation method thereof. A novel intermediate is introduced into the eribulin synthesis route, which comprises more than 60 steps. The advantages of various routes in the prior art are integrated so as to industrially produce (macro-cyclic ketone) eribulin, which is difficult to synthesize.

The present invention relates to a method for preparing eribulin and an intermediate thereof. In particular, the invention relates to a method for preparing a compound of formula 5, R3 is selected from aldehyde or OR1, n=0 or 1, R1 is a hydroxy protecting group, and preferably the hydroxy protecting group is selected from tert-butyldimethylsilyl, tert-butyldiphenylsilyl, p-methoxybenzyl or benzyl.The invention also provides a method for preparing halichondrin and derivatives thereof such as the eribulin from the compound of formula 5.

The invention provides a compound and a preparation method and application thereof. The preparation method comprises the following steps: firstly, transforming a compound with a structure shown as a formula (III) into an intermediate with a structure shown as a formula (II); transforming the intermediate with the structure shown as the formula (II) into a compound with a structure shown as a formula (IV); then, transforming the compound shown as the formula (IV) into eribulin. In a synthetic route, the reaction yield is high, so that the total yield of the synthesized eribulin is increased.

The invention discloses a synthesis method of an eribulin intermediate. The synthesis method mainly comprises the following steps: taking a compound shown as a formula 1 as a raw material to react with N-iodosuccinimide and then carrying out hydroxyl protection reaction to obtain a target product, namely a compound shown as a formula 4. The synthesis method provided by the technical scheme has theadvantages of simple and convenient operation steps, moderate reaction conditions and a few of byproducts in a reaction process; compared with the prior art, the productivity and the yield of the target product are remarkably improved and the synthesis method is very suitable for industrial production.

The invention provides methods of treating breast cancer in subjects having locally advanced or metastatic breast cancer.

The present disclosure describes combination therapies comprising an antagonist of Programmed Death 1 receptor (PD- 1 ) and eribulin or a pharmaceutically acceptable salt thereof, and the use of the combination therapies for the treatment of cancer.

The present invention provides methods and compositions for treating cancers with a combination of eribulin and a selective CDK4/6 inhibitor, wherein the selective CDK4/6 inhibitor reduces eribulin's effects on myelosuppression and/or myeloablation without reducing the efficacy of eribulin therapy.

The invention provides a preparation method of an eribulin intermediate. According to the preparation method, a brand-new route and an intermediate are adopted to prepare a key intermediate ERB, compared with the prior art, the reaction route is greatly simplified, the reaction yield and the selectivity of a new chiral center of a target product are remarkably improved; and the preparation methodis especially suitable for industrial application.

The present disclosure describes combination therapies comprising an antagonist of Programmed Death 1 receptor (PD-1) and eribulin or a pharmaceutically acceptable salt thereof, and the use of the combination therapies for the treatment of urothelial cancer.

The invention discloses a synthetic method of an eribulin intermediate ER806047 shown as a formula (b), comprising the following steps of: using 1, 2-O-isopropylidene-alpha-D-glucuronic acid-6, 3-lactone as a raw material, and carrying out one-step oxidation-reduction reaction for dehydroxylation synthesis of the eribulin intermediate ER806047. The synthetic method has the advantages of short reaction route, high yield, simplicity and convenience in operation, low cost, suitability for industrial production and the like. The structure of the eribulin intermediate ER806047 disclosed by the invention is as shown in the specification.

The present invention provides a novel liposome composition containing eribulin or its pharmacologically permissible salt, and its method of manufacture.

Discloses is a process for preparation of a compound of formula 7, or a derivative thereof, wherein PG¹ is an alcohol protecting group. Also, disclosed are intermediates and processes for their preparation. The compound of formula 7 can be useful in the preparation of halinchondrin analogs such as Eribulin.

The invention relates to a preparation method of an eribulin intermediate, concretely relates to a compound represented by formula III, formula IV or formula X (R<1> is an alkyl group or a substitutedor unsubstituted aryl group), and especially relates to a preparation method of the compound represented by formula III, formula IV or formula X. The method has the advantages of mild reaction conditions, simplicity in operation, and low synthesis cost, and is suitable for large-scale production.

The invention belongs to the field of drug synthesis, and particularly relates to an eribulin intermediate and a synthesis method and application thereof. The invention provides an intermediate whichcan be used for synthesizing halichondrin B, eribulin or analogues thereof, particularly C27-C35 structural fragments thereof, as well as a preparation method and application of the intermediate. Theinitial raw materials of the synthetic route are cheap and easy to obtain, and the optical purity of the synthetic route can be guaranteed so that the optical purity of C27-C35 structural fragments inhalichondrin, eribulin or analogues thereof is guaranteed; according to the method, the chiral center of the C27-C35 structural fragment is constructed, the diastereoselectivity and yield are high, and especially the preparation method of the compounds shown in the formula (X), the formula (XI), the formula (XVI) and the formula (XV) is provided; partial reaction by-products can be removed only by recrystallization so that purification is facilitated, and the cost is greatly reduced.