Treprostinil is a synthetic prostacyclin derivative with thrombocyte aggregation inhibitory and vasodilatory activity. Treprostinil can be administered in subcutaneous, intravenous, inhalable, or oral forms. Disclosed is a method for the preparation of treprostinil of formula I and its amorphous form, anhydrate form, monohydrate form, and polyhydrate form salts with bases. In the disclosed method, the chiral center in the 3-hydroxyoctyl substituent is formed at the end of the synthesis, so that the method is robust and well scalable.

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Also disclosed are treprostinil intermediates and the preparation of the intermediates.

Treprostinil is a synthetic prostacyclin derivative with thrombocyte aggregation inhibitory and vasodilatory activity. Treprostinil can be administered in subcutaneous, intravenous, inhalable, or oral forms. Disclosed is a method for the preparation of treprostinil of formula I and its amorphous form, anhydrate form, monohydrate form, and polyhydrate form salts with bases. In the disclosed method, the chiral center in the 3-hydroxyoctyl substituent is formed at the end of the synthesis, so that the method is robust and well scalable.

##STR00001##

Also disclosed are treprostinil intermediates and the preparation of the intermediates.

Treprostinil is a synthetic prostacyclin derivative with thrombocyte aggregation inhibitory and vasodilatory activity. Treprostinil can be administered in subcutaneous, intravenous, inhalable, or oral forms. Disclosed is a method for the preparation of treprostinil of formula I and its amorphous form, anydrate form, monohydrate form, and polyhydrate form salts with bases. In the disclosed method, the chiral center in the 3-hydroxyoctyl substituent is formed at the end of the synthesis, so that the method is robust and well scalable. ##STR00001##
Also disclosed are treprostinil intermediates and the preparation of the intermediates.

Treprostinil is a synthetic prostacyclin derivative with thrombocyte aggregation inhibitory and vasodilatory activity. Treprostinil can be administered in subcutaneous, intravenous, inhalable, or oral forms. Disclosed is a method for the preparation of treprostinil of formula I and its amorphous form, anydrate form, monohydrate form, and polyhydrate form salts with bases. In the disclosed method, the chiral center in the 3-hydroxyoctyl substituent is formed at the end of the synthesis, so that the method is robust and well scalable. ##STR00001##
Also disclosed are treprostinil intermediates and the preparation of the intermediates.

An organic compound, a three-dimensional organic structure formed by using the organic compound, a separation sieve and an optical layer having the organic structure, and an optical device having the optical layer as an optical amplification layer are provided. The organic structure includes a plurality of organic molecules self-assembled by non-covalent bonding. Each of the unit organic molecules has an aromatic ring, a first pair of substituents being connected to immediately adjacent positions of substitutable positions of the aromatic ring, and a second pair of substituents being connected to immediately adjacent positions of remaining substitutable positions of the aromatic ring. The unit organic molecules are self-assembled by van der Waals interaction, London dispersion interaction or hydrogen bonding between the first and the second pairs of the substituents and by pi-pi interactions between the aromatic rings.

Provided are compounds of formulae provided herein. The compounds may include pathway-preferential estrogens (PaPEs) derivatives with tissue-selective activities. Also provided are pharmaceutical compositions comprising the compounds, as well as methods of treating a disease or condition including administering the compounds. The disease or condition may include postmenopausal symptoms, cardiovascular disease, stroke, vascular disease, bone disease, metabolic disease, arthritis, osteoporosis, obesity, vasomotor/hot flush, cognitive decline, cancer including breast cancer.

Methods of CH bond fluorination using non-heme manganese catalyst are described herein. For example, a method comprises providing a reaction mixture including a non-heme manganese catalyst, a substrate comprising an sp.sup.3 CH bond and a fluorinating agent and converting the sp.sup.3 CH bond to a CF bond in the presence of the non-heme manganese catalyst or a derivative thereof.

Methods of CH bond fluorination using non-heme manganese catalyst are described herein. For example, a method comprises providing a reaction mixture including a non-heme manganese catalyst, a substrate comprising an sp.sup.3 CH bond and a fluorinating agent and converting the sp.sup.3 CH bond to a CF bond in the presence of the non-heme manganese catalyst or a derivative thereof.

The present invention provides a small molecule TNF-? inhibitor STU104 and a preparation method and use thereof, wherein an absolute configuration of an optical isomer (R)-STU104 is identified, especially it has found use of STU104 for treatment of autoimmune inflammatory diseases mediated due to TNF-? overexpression including ulcerative colitis, Crohn's disease, rheumatoid arthritis, osteoarthritis, alopecia areata, Sjogren's syndrome, lupus erythematosus, dermatomyositis, etc. The present invention has broad clinical therapeutic significance.

The present invention provides a small molecule TNF-? inhibitor STU104 and a preparation method and use thereof, wherein an absolute configuration of an optical isomer (R)-STU104 is identified, especially it has found use of STU104 for treatment of autoimmune inflammatory diseases mediated due to TNF-? overexpression including ulcerative colitis, Crohn's disease, rheumatoid arthritis, osteoarthritis, alopecia areata, Sjogren's syndrome, lupus erythematosus, dermatomyositis, etc. The present invention has broad clinical therapeutic significance.