80 results about "Fondaparinux Sodium" patented technology

The invention relates to fondaparinux sodium, intermediates thereof and preparation methods in the technical field of chemical preparation, particularly relates to the preparation methods of the fondaparinux sodium and the intermediates of the fondaparinux sodium, comprising the fondaparinux sodium, a disaccharide intermediate of the fondaparinux sodium, a tetrasccharide intermediate of the fondaparinux sodium, a pentasaccharide intermediate of the fondaparinux sodium and the corresponding preparation methods. The structure of the fondaparinux sodium is shown as the chemical compound (1). The invention also relates to the disaccharide intermediate, the tetrasccharide intermediate and the pentasaccharide intermediate which are used for preparing the fondaparinux sodium. The invention designs a novel synthetic route to prepare the fondaparinux sodium. The novel synthetic route has mild reactions, good reaction selectivity, strong controllability and low operation difficulty, and is prone to achievement of industrial production.

The present invention provides novel processes for the preparation of Fondaparinux sodium by using the compound of formula ABC5In some embodiments, the intermediates for the synthesis of Fondaparinux sodium, are also provided.

The invention relates to a novel technology for preparing disaccharide fragment of an anticoagulant drug fondaparinux sodium intermediate. The technology has the advantages of short reaction route, high efficiency, and easy purifying of the intermediate, and is suitable for commercial production of the full protection heparin pentasaccharide.

The invention relates to a Fondaparinux sodium composition injection and a preparation method thereof. The injection is prepared from raw materials as follows: 5-10 parts by mass of Fondaparinux sodium, 6-12 parts by mass of sodium chloride, 2.6-3 parts by mass of a buffer solution and 3-6 parts by volume of water for injection, wherein the buffer solution is a mixture of citric acid, sodium hydroxide and hydrochloric acid, and a mass ratio of citric acid, sodium hydroxide and hydrochloric acid is (2.4-2.6):1:(1.3-1.9); the raw materials are subjected to orderly feeding, stirring, filtering, reflowing, filling, nitrogen charge, fused sealing, high-temperature sterilization, light inspection after cooling, packaging and checking, and the Fondaparinux sodium composition injection is obtained. The Fondaparinux sodium composition injection prepared with the method cannot produce crystals, is good in clarity, greatly improves the stability and is better applied to clinical treatment.

The invention discloses a separation extraction method of fondaparinux sodium. The method includes the following steps: adsorbing a dilute salt solution of a fondaparinux sodium compound by ion exchange resin, then eluting with concentrated brine solution to achieve the purpose of salt removal and concentration, so as to obtain concentrated liquid of fondaparinux sodium. The invention uses ion exchange resin before fondaparinux sodium adsorption, to separate most of the salt and water, and then a small amount of concentrated brine solution is employed to elute the product, and the subsequent precipitation is carried out directly to obtain the product. The method is simple and practical in operation and low in cost and can control processing batch arbitrarily, so as to greatly facilitate the posttreatment process of the fondaparinux sodium product.

The present invention describes an analytical method for detecting and quantitating poly-sulfated oligosaccharides, including Fondaparinux sodium, using hydrophilic interaction ultra-performance liquid chromatography (HILIC-UPLC) coupled with a charged aerosol detector (CAD) or a mass spectrometer (MS). This analytical method provides in-process control in a total synthesis of highly sulfated oligosaccharides by separation, quantification and mass identification. Systems and conditions utilizing such methods are also provided.

The invention discloses a preparation method of a fondaparinux sodium injection composition. The preparation method comprises the following steps of 1) according to a prescription of the fondaparinuxsodium injection composition, weighing all materials by prescription dosage; 2) taking fondaparinux sodium and sodium chloride, combining, then adding injection water with the weight being 75-85% of the total weight, after stirring and dissolving, adopting a pH regulator to regulate the pH to 5-8, then adding remaining injection water, stirring and mixing uniformly to obtain liquid medicine; 3) filling prepared liquid medicine, and carrying out high-temperature sterilization, cooling, lamp inspection, package and inspection to obtain the fondaparinux sodium injection composition. The fondaparinux sodium injection composition prepared by the invention has the advantages that by optimizing the pH and sterilization process of the fondaparinux sodium injection composition, the obtained solution is good in clarity and conforms to all detection requirements of the injection liquid item in Chinese pharmacopoeia, so that the quality stability of products is greatly improved, the crystallization and the turbidity of the solution are reduced, and the generation of impurities is reduced.

The invention relates to a compound as shown in formula I for preparing fondaparinux sodium, a preparation method thereof and a preparation method of the fondaparinux sodium. The compound disclosed by the invention can be prepared from raw materials which are easy to obtain at higher selectivity and yield, thereby greatly simplifying the preparation process of the fondaparinux sodium. The definition of various substitutional groups contained in the formula I is the same as the definition in a specification.

The present invention discloses novel devices, methods, and formulations for multiple dose delivery of an appropriate formulation of Heparin or low molecular weight heparin or a heparin-like compound. Multiple dose formulations of fondaparinux sodium, and preparation methods thereof, are also disclosed

The invention discloses a fondaparinux sodium disaccharide intermediate preparation method which comprises the following steps: firstly, using a formula (II) compound and a formula (III) compound for preparation of a formula (IV) compound; then using the prepared formula (IV) compound for the preparation of a formula (I) compound. The technical scheme of the fondaparinux sodium disaccharide intermediate preparation method is low in cost and high in yield, raw materials are easy to prepare, and by use of the intermediate as a raw material for preparation of fondaparinux, the cost can be greatly reduced.

The present invention relates to a process for the synthesis of the Factor Xa anticoagulent Fondaparinux and related compounds. The invention relates, in addition, to efficient and scalable processes for the synthesis of various intermediates useful in the synthesis of Fondaparinux and related compounds.

The invention relates to an automatic preparation method of a fondaparinux sodium pentasaccharide intermediate. The method is based on an automatic preparation device. According to the method, automatic preparation of three components (D+EF+GH) is realized through automatic sample injection and automatic sampling and monitoring, the fully-protected fondaparinux sodium pentasaccharide intermediate(formula I) is obtained, and automatic synthesis of the fondaparinux sodium pentasaccharide intermediate is realized, so that the manpower can be saved, the efficiency and productivity are improved, and relatively high safety and reproducibility are achieved; direct online monitoring can be realized, the real-time state of a reaction is convenient to optimize and monitor, and meanwhile, the automatic temperature control can better meet the requirements of the reaction on heating and cooling; a pre-activation one-kettle mode is adopted, so that the separation frequency is reduced, and the operation is convenient; and a common ester protecting group is selected, relatively high stereoselectivity and yield are achieved, a universal deprotection method can be used, and the method has importantsignificance in reducing the production cost of fondaparinux sodium and achieving large-scale production. The definition of each substituent in the formula I is the same as the definition in the specification.