50 results about "Cyclooctanes" patented technology

The invention provides novel 8-azabicyclo[3.2.1]octane compounds of formula (I):wherein R1, R2, R3, A, and G are defined in the specification, or a pharmaceutically-acceptable salt or solvate thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.

The invention discloses a method for synthesizing (2S,3S)-3-amino-bicyclo[2.2.2] octane-2-formate and belongs to the field of pharmaceutical intermediate synthesis. The purposes of the invention are to solve the problems of high preparation cost, low material safety and the like of (2S, 3S)-3-amino-bicyclo[2.2.2] octane-2-formate, further improve the productivity and reduce the production cost. According to the method disclosed by the invention, 3-carbonyl-bicyclo[2.2.2] octane-2-formate is used as a starting material, and reductive amination, basic configuration inversion, hydrogenation protection group removal and the like are sequentially carried out, so that the target product is obtained. According to the invention, the (2S, 3S)-3-amino-bicyclo [2.2. 2] octane-2-formate is synthesizedby using the synthesis method, the novel process route is used, the yield is more than 65%, and the method has characteristics of novel route, mild reaction condition, low cost and the like.

Benzobicyclooctane compounds, their use in inhibiting cellular events involving TNF-α and IL-8, and in the treatment of inflammation events in general; a combinatorial library of diverse bicyclooctanes and process for their synthesis as a library and as individual compounds.

The invention discloses a 2,6-dioxobicyclo[3.3.2]octane derivative and a synthesis method thereof. The synthesis method of the derivative is based on (E)-2-hydroxyl-1-naphthalene vinyl derivative The substrate is under the action of 1-chloromethyl-4-fluoro-1, 4-diazotized bicyclo[2.2.2]octane bis(tetrafluoroborate) salt and cuprous chloride, and the reaction obtains a novel 2,6-Dioxobicyclo[3.3.2]octane skeleton derivative compound. The method of the invention is simple to operate, and the reaction conditions are mild, and a novel 3D skeleton, two rings, three new chemical bonds (two C-O, one C-C) and four chiral centers are constructed in a one-pot reaction And a single stereo configuration was obtained, and a series of 2,6-dioxobicyclo[3.3.2]octane derivatives were constructed.

The invention discloses a divalent manganese fluorescent material based on dibromo-1,4-dipropyl-1,4-diazabicyclo[2.2.2]octane and its preparation method and application, belonging to molecular ion-based Divalent manganese fluorescent material. The chemical formula of the fluorescent material is C12H26N2Cl4Mn. At the temperature of 296K, the crystal belongs to the orthorhombic system, and the chiral space group is P212121. The product is prepared by mixing soluble salts containing Mn2+ and triethylenediamine derivatives and self-assembling with natural volatile solvents of the solution. The material preparation process adopted by the fluorescent material of the present invention is simple, easy to operate, sufficient source of raw materials, low production cost, high yield and good repeatability; the thermal decomposition temperature point is relatively high, and the crystal particles are uniform.

The invention relates to an alkaline anion-exchange membrane fuel cell, in particular to a cross-linked polybenzimidazole alkaline anion-exchange membrane and its preparation and application. The method includes the synthesis of N1-long-chain alkane-substituted-1,4-diazabicyclo[2.2.2]octane, N1-long-chain alkane-substituted-1,4-diazabicyclo[2.2.2] Preparation of Octane-functionalized Polybenzimidazole‑Polyvinylbenzyl Chloride Crosslinked Basic Anion Exchange Membranes. The invention adopts the homogeneous method to prepare the crosslinked anion exchange membrane, and the crosslinking and quaternization are completed in one step, which is simple and efficient, not only improves the mechanical strength and dimensional stability of the crosslinked membrane, but also effectively improves the homogeneous reaction used in the preparation process. The efficiency of quaternization is improved, and the microscopic phase separation structure in the membrane makes the crosslinked membrane have high conductivity, and has the advantages of excellent dimensional stability and chemical stability, etc., and has potential in alkaline anion exchange membrane fuel cells. application prospects.

The invention discloses a method for synthesizing a Bictegravir intermediate. The starting material 3-carbonyl cyclopentanecarboxylic acid (formula I) undergoes an asymmetric reduction reaction under the condition of an enzyme to generate (3R)-3-hydroxycyclopentane Carboxylic acid (Formula II); Formula II reacts with diphenylphosphoryl azide (DPPA) to generate (1R,5S)‑2‑Oxy‑4‑azabicyclo[3.2.1]octane -3-ketone (formula III); formula III is hydrolyzed in hydrochloric acid to directly obtain the Bictegravir intermediate (1R,3S)-3-aminocyclopentanol hydrochloride. The raw materials used in the present invention are cheap and easy to obtain, and the cost is low; the reaction selectivity is high, the by-products are few, the yield is high, and the total yield reaches 63.5%; Hydrogen pressurized reduction and Grignard reagent reaction are adopted, which is safe and environmentally friendly, and suitable for industrial production.

The invention discloses a method for preparing chiral 3,6-diazabicyclo[3.2.1]octane derivatives. The chiral 3,6-diazabicyclo[3.2.1]octane The derivatives synergistically catalyze the 1,3-dipolar cycloaddition reaction between different series of azomethine ylides and α-substituted terminal olefin amides through monovalent silver salts combined with different chiral phosphine-amide ligands. Chiral 3,6‑diazabicyclo[3.2.1]octane derivatives were directly obtained by intramolecular cyclization under strong base treatment. The preparation method of the invention has simple steps, relatively cheap and easy-to-obtain raw materials, low corrosion and low toxicity, and simple and easy-to-realize reaction conditions. The 3,6-diazabicyclo[3.2.1]octane derivative obtained according to the preparation method of the chiral 3,6-diazabicyclo[3.2.1]octane derivative can be applied to medicine Inhibitors or drug intermediates.

The present invention relates to a pharmaceutical composition and a lyophilisate of a diazabicyclooctane derivative represented by Compound I, a process for producing the same and methods for using the same.