Novel compounds that find use as imaging agents within nuclear medicine applications (PET imaging) for imaging of cardiac innervation are disclosed. These PET based radiotracers may exhibit increased stability, decreased NE release (thereby reducing side effects), improved quantitative data, and/or high affinity for VMAT over prior radiotracers. Methods of using the compounds to image cardiac innervation are also provided. In some instances the compounds are developed by derivatizing certain compounds with 18F in a variety of positions: aryl, alkyl, a keto, benzylic, beta-alkylethers, gamma-propylalkylethers and beta-proplylalkylethers. Alternatively or additionally, a methyl group a is added to the amine, and/or the catechol functionality is either eliminated or masked as a way of making these compounds more stable.

Subject-matter of the present invention is a process for the preparation of optically active phenyl-beta-amino alcohols by means of a specific reduction of the corresponding phenyl-beta-amino ketones. Further subject-matter of the invention are said novel synthesis intermediates and their use for the preparation of active pharmaceutical ingredients.

Subject-matter of the present invention is a process for the preparation of optically active phenyl-beta-amino alcohols by means of a specific reduction of the corresponding phenyl-beta-amino ketones. Further subject-matter of the invention are said novel synthesis intermediates and their use for the preparation of active pharmaceutical ingredients.

The present invention relates to systems, compositions, and methods for the synthesis and use of imaging agents, or precursors thereof. An imaging agent precursor may be converted to an imaging agent using the methods described herein. In some cases, the imaging agent is enriched in .sup.18F. In some cases, an imaging agent may be used to image an area of interest in a subject, including, but not limited to, the heart, cardiovascular system, cardiac vessels, brain, and other organs. In some embodiments, methods and compositions for assessing perfusion and innervation mismatch in a portion of a subject are provided.

The present invention relates to systems, compositions, and methods for the synthesis and use of imaging agents, or precursors thereof. An imaging agent precursor may be converted to an imaging agent using the methods described herein. In some cases, the imaging agent is enriched in .sup.18F. In some cases, an imaging agent may be used to image an area of interest in a subject, including, but not limited to, the heart, cardiovascular system, cardiac vessels, brain, and other organs. In some embodiments, methods and compositions for assessing perfusion and innervation mismatch in a portion of a subject are provided.

Provided herein are compounds of Formula (I), or pharmaceutically acceptable salt thereof, wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, and n are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I) or pharmaceutically acceptable salt thereof, and methods of using a compound of Formula (I) or pharmaceutically acceptable salt thereof, e.g., in the treatment of a mental health disease or disorder. ##STR00001##

A method for preparing R-terbutaline by using a chiral auxiliary uses S-(?)-tert-butylsulfinamide as a starting material to sequentially react with tert-butylbromide and 1-(3,5-bis(benzyloxy)phenyl)-2-bromoethan-1-one to obtain a compound 5; the compound 5 is subjected to a reduction reaction under the catalysis of a quaternary ammonium salt to obtain a compound 6; the tert-butylsulfinyl group of compound 6 is deprotected to obtain a compound 7, and in the presence of a palladium catalyst and hydrochloric acid, the compound 7 is hydrogenolyzed in an alcohol solvent to obtain the R-terbutaline. The method is simple and reliable, the preparation costs are low, and the ee of the chiral product is as high as 99.9%.

A method for preparing R-terbutaline by using a chiral auxiliary uses S-(?)-tert-butylsulfinamide as a starting material to sequentially react with tert-butylbromide and 1-(3,5-bis(benzyloxy)phenyl)-2-bromoethan-1-one to obtain a compound 5; the compound 5 is subjected to a reduction reaction under the catalysis of a quaternary ammonium salt to obtain a compound 6; the tert-butylsulfinyl group of compound 6 is deprotected to obtain a compound 7, and in the presence of a palladium catalyst and hydrochloric acid, the compound 7 is hydrogenolyzed in an alcohol solvent to obtain the R-terbutaline. The method is simple and reliable, the preparation costs are low, and the ee of the chiral product is as high as 99.9%.

The present disclosure relates generally to methods for the preparation of Compound (I).

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The present disclosure relates generally to methods for the preparation of Compound (I).

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