The present disclosure provides acetate salts of buprenorphine, and its anhydrates, solvates, hydrates, and crystalline forms thereof, where the acetate salts of buprenorphine are essentially free of impurities. The disclosure further provides method of preparing the acetate salts, buprenorphine free base prepared from the acetate salts, other salts prepared from the free base, and pharmaceutical compositions thereof essentially free of impurities.

The present invention provides a process for the preparation of a compound of formula (2): the process comprising reacting a compound of formula (1), a base and an alkylating agent R.sub.4X in a nitrile-containing polar aprotic solvent to form the compound of formula (2), wherein the process is carried out at a temperature greater than 60 C.; and wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, and X are as defined in the specification.

##STR00001##

The present invention provides a process for the preparation of a compound of formula (2): the process comprising reacting a compound of formula (1), a base and an alkylating agent R.sub.4X in a nitrile-containing polar aprotic solvent to form the compound of formula (2), wherein the process is carried out at a temperature greater than 60 C.; and wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, and X are as defined in the specification.

##STR00001##

The present disclosure provides acetate salts of buprenorphine, and its anhydrates, solvates, hydrates, and crystalline forms thereof, where the acetate salts of buprenorphine are essentially free of impurities. The disclosure further provides method of preparing the acetate salts, buprenorphine free base prepared from the acetate salts, other salts prepared from the free base, and pharmaceutical compositions thereof essentially free of impurities.

The present disclosure provides acetate salts of buprenorphine, and its anhydrates, solvates, hydrates, and crystalline forms thereof, where the acetate salts of buprenorphine are essentially free of impurities. The disclosure further provides method of preparing the acetate salts, buprenorphine free base prepared from the acetate salts, other salts prepared from the free base, and pharmaceutical compositions thereof essentially free of impurities.

The present invention relates to a compound represented by formula I and a non-toxic pharmaceutically acceptable salt thereof. In formula (I), R1 is H, CH.sub.3 or deuterated methyl (CD.sub.3); R2 is CH.sub.3 or CH.sub.2CH.sub.3; R3, R4 and R5 are each independently H or deuterium (D); when R1 is H or CH.sub.3, at least one of R3, R4 and R5 is D. ##STR00001##

The present invention relates to a compound represented by formula I and a non-toxic pharmaceutically acceptable salt thereof. In formula (I), R1 is H, CH.sub.3 or deuterated methyl (CD.sub.3); R2 is CH.sub.3 or CH.sub.2CH.sub.3; R3, R4 and R5 are each independently H or deuterium (D); when R1 is H or CH.sub.3, at least one of R3, R4 and R5 is D. ##STR00001##

A device and method utilizing user operated actuators such as momentary switches, intermediate switches, accelerometers or video cameras to detect impaired consciousness as an early symptom of opioid overdose to then trigger administration of preloaded naloxone to rescue the user from an overdose.

The present invention relates to a compound represented by formula I and a non-toxic pharmaceutically acceptable salt thereof. In formula (I), R1 is H, CH.sub.3 or deuterated methyl (CD.sub.3); R2 is CH.sub.3 or CH.sub.2CH.sub.3; R3, R4 and R5 are each independently H or deuterium (D); when R1 is H or CH.sub.3, at least one of R3, R4 and R5 is D.

##STR00001##

The present invention relates to a compound represented by formula I and a non-toxic pharmaceutically acceptable salt thereof. In formula (I), R1 is H, CH.sub.3 or deuterated methyl (CD.sub.3); R2 is CH.sub.3 or CH.sub.2CH.sub.3; R3, R4 and R5 are each independently H or deuterium (D); when R1 is H or CH.sub.3, at least one of R3, R4 and R5 is D.

##STR00001##